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Banasri Hazra - One of the best experts on this subject based on the ideXlab platform.

  • D and Hazra B (2000) Effects of atovaquone and Diospyrin-based drugs on ubiquinone biosynthesis in Pneumocystis carinii organisms. Antimicrob Agents Chemother
    2016
    Co-Authors: Edna Kaneshiro, Banasri Hazra, Edna S. Kaneshiro, Donggeun Sul
    Abstract:

    The naphthoquinone atovaquone is effective against Plasmodium and Pneumocystis carinii carinii. In Plas-modium, the primary mechanism of drug action is an irreversible binding to the mitochondrial cytochrome bc1 complex as an analog of ubiquinone. Blockage of the electron transport chain ultimately inhibits de novo pyrimidine biosynthesis since dihydroorotate dehydrogenase, a key enzyme in pyrimidine biosynthesis, is un-able to transfer electrons to ubiquinone. In the present study, the effect of atovaquone was examined on Pneu-mocystis carinii carinii coenzyme Q biosynthesis (rather than electron transport and respiration) by measuring its effect on the incorporation of radiolabeled p-hydroxybenzoate into ubiquinone in vitro. A triphasic dose-response was observed, with inhibition at 10 nM and then stimulation up to 0.2 mM, followed by inhibition at 1 mM. Since other naphthoquinone drugs may also act as analogs of ubiquinone, Diospyrin and two of its de-rivatives were also tested for their effects on ubiquinone biosynthesis in P. carinii carinii. In contrast to atova-quone, these drugs did not inhibit the incorporation of p-hydroxybenzoate into P. carinii carinii ubiquinone. Ubiquinone (coenzyme Q [CoQ]) (Fig. 1A) plays a pivota

  • Antimycobacterial activity of Diospyrin and its derivatives against Mycobacterium aurum
    2015
    Co-Authors: Stanley Mukanganyama, Elaine Chirisa, Banasri Hazra
    Abstract:

    The objective of this study was to determine the antimycobacterial activity of Diospyrin (D1) and four of its derivatives (D2, D5, D7 and D17) against the non-pathogenic Mycobacterium aurum. The effect of these compounds was determined on growth parameters and drug efflux pumping activity. Diospyrin was shown to be the most active in inhibiting the growth of M. aurum whilst D2 was inactive. D17 was found to have the lowest MIC of < 0.1 µg/ml, while the MIC of other compounds were found to be as follows: D1= 0.1 µg/ml, D5= 0.39 µg/ml, D7= 0.78 µg/ml and D2 =3.13 µg/ml, in order of potency. The compounds were bacteriostatic rather than bactericidal as the MBCs were greater than 50 µg/ml. The compounds were potent efflux pump inhibitors as D5 enhanced ciprofloxacin accumulation by 160 %, D17 by 58 %, D7 by 41 %, D1 by 37 % when compared with the standard efflux pump inhibitor, reserpine, which enhanced accumulation by 51 %. D2 had no effect on drug efflux pumping activity. The modifications of Diospyrin enhanced the activity of D17 and D5 by decreasing the MIC and enhancing accumulation of ciprofloxacin, respectively. In contrast, activity decreased significantly for D2 in the growth and accumulation assays. Diospyrin and its derivatives are potential antimycobacterial agents and drug efflux inhibitors and could be used to enhance the activity of known antimycobacterial agents that are actively effluxed from M. tuberculosis.

  • Acetylamine derivative of Diospyrin, a plant-derived binaphthylquinonoid, inhibits human colon cancer growth in Nod-Scid mice
    Investigational New Drugs, 2015
    Co-Authors: Sudipta Hazra, Subhalakshmi Ghosh, Amit Kumar, B. N. Pandey, Banasri Hazra
    Abstract:

    Anticancer activity of Diospyrin and its derivatives ( 1 – 5 ) was evaluated against thirteen human cell lines. Compared to Diospyrin ( 1 ), the acetylamine derivative ( 4 ) exhibited increase in cytotoxicity, particularly in HT-29 colon cancer cells, showing GI_50 values of 33.90 and 1.96 μM, respectively. Also, enhanced toxicity was observed when cells, pre-treated with compound 4 , were exposed to radiation. In vivo assessment of 4 was undertaken on tumour-bearing Nod -Scid mice treated at 4 mg/kg/day. Significant reduction in relative tumour volume (~86–91 %) was observed during the 12th–37th days after drug treatment. Increased caspase-3 activity and DNA ladder formation was observed in HT-29 cells after treatment with 4 , suggesting induction of apoptotic death after drug treatment. Moreover, flow cytometric determination of Annexin V- FITC positive and PI negative cells demonstrated 17.4, 26.4, and 27.9 % of early apoptosis, respectively, upon treatment with 5, 10 and 25 μM of 4 . HT-29 cells after treatment with 4 (1–25 μM) revealed ~2.5- 3- folds generation of ROS. Furthermore, concentration dependent decrease of mitochondrial trans-membrane potential (∆ψ_m), and expression of Bcl-2/Bax and other marker proteins suggested involvement of mitochondrial pathway of cell death. Overall, our results demonstrated the underlying cell-death mechanism of the plant-derived naphthoquinonoid ( 4 ), and established it as a prospective chemotherapeutic ‘lead’ molecule against colon cancer.

  • antitubercular and antibacterial activity of quinonoid natural products against multi drug resistant clinical isolates
    Phytotherapy Research, 2014
    Co-Authors: Diganta Dey, Ratnamala Ray, Banasri Hazra
    Abstract:

    Multi-drug resistant Mycobacterium tuberculosis and other bacterial pathogens represent a major threat to human health. In view of the critical need to augment the current drug regime, we have investigated therapeutic potential of five quinonoids, viz. emodin, Diospyrin, plumbagin, menadione and thymoquinone, derived from natural products. The antimicrobial activity of quinonoids was evaluated against a broad panel of multi-drug and extensively drug-resistant tuberculosis (M/XDR-TB) strains, rapid growing mycobacteria and other bacterial isolates, some of which were producers of β-lactamase, Extended-spectrum β-lactamase (ESBL), AmpC β-lactamase, metallo-beta-lactamase (MBL) enzymes, as well as their drug-sensitive ATCC counterparts. All the tested quinones exhibited antimycobacterial and broad spectrum antibacterial activity, particularly against M. tuberculosis (lowest MIC 0.25 µg/mL) and Gram-positive bacteria (lowest MIC  emodin ~ menadione ~ thymoquinone > Diospyrin, whereas their antibacterial efficacy was plumbagin > menadione ~ thymoquinone > Diospyrin > emodin. Furthermore, this is the first evaluation performed on these quinonoids against a broad panel of drug-resistant and drug-sensitive clinical isolates, to the best of our knowledge. Copyright © 2013 John Wiley & Sons, Ltd.

  • Evaluation of a Diospyrin derivative as antileishmanial agent and potential modulator of ornithine decarboxylase of Leishmania donovani
    Experimental parasitology, 2013
    Co-Authors: Sudipta Hazra, Madhushree Das Sarma, Subhalakshmi Ghosh, Smriti Sharma, Mousumi Das, Prakash Saudagar, Vijay Kumar Prajapati, Vikash Kumar Dubey, Shyam Sundar, Banasri Hazra
    Abstract:

    Abstract World health organization has called for academic research and development of new chemotherapeutic strategies to overcome the emerging resistance and side effects exhibited by the drugs currently used against leishmaniasis. Diospyrin, a bis-naphthoquinone isolated from Diospyros montana Roxb., and its semi-synthetic derivatives, were reported for inhibitory activity against protozoan parasites including Leishmania. Presently, we have investigated the antileishmanial effect of a di-epoxide derivative of Diospyrin (D17), both in vitro and in vivo. Further, the safety profile of D17 was established by testing its toxicity against normal macrophage cells (IC50 ∼ 20.7 μM), and also against normal BALB/c mice in vivo. The compound showed enhanced activity (IC50 ∼ 7.2 μM) as compared to Diospyrin (IC50 ∼ 12.6 μM) against Leishmania donovani promastigotes. Again, D17 was tested on L. donovani BHU1216 isolated from a sodium stibogluconate-unresponsive patient, and exhibited selective inhibition of the intracellular amastigotes (IC50 ∼ 0.18 μM). Also, treatment of infected BALB/c mice with D17 at 2 mg/kg/day reduced the hepatic parasite load by about 38%. Subsequently, computational docking studies were undertaken on selected enzymes of trypanothione metabolism, viz. trypanothione reductase (TryR) and ornithine decarboxylase (ODC), followed by the enzyme kinetics, where D17 demonstrated non-competitive inhibition of the L. donovani ODC, but could not inhibit TryR.

Amalendu Banerjee - One of the best experts on this subject based on the ideXlab platform.

  • pharmacological studies on the effect of the treatment of swiss a mice with Diospyrin a tumour inhibitory plant product and its synthetic derivatives
    Phytotherapy Research, 1996
    Co-Authors: Sampa Pal, Banasri Hazra, Ratnamala Ray, Amalendu Banerjee, Dilip K. Bhattacharya
    Abstract:

    Diospyrin, a bisnaphthoquinonoid plant product and its derivatives have shown significant inhibitory activities against murine tumours in vivo. Studies on the haematological status, serum protein and creatinine levels, activities of several serum glycolytic enzymes, and histopathology of the mice inoculated with Ehrlich ascites carcinoma were carried out after treatment with Diospyrin and four synthetic derivatives. The prognostic significance of the pharmacological parameters acting as markers of the diseased state was evident from these findings. Normal mice were also studied before and after treatment with these compounds which did not cause noticeable adverse effects on the vital parameters, thereby indicating the possibility of the utilization of Diospyrin and derivatives as appropriate therapeutic agents.

  • Pharmacological Studies on the Effect of the Treatment of Swiss A Mice with Diospyrin, a Tumour‐inhibitory Plant Product, and its Synthetic Derivatives
    Phytotherapy Research, 1996
    Co-Authors: Sampa Pal, Banasri Hazra, Ratnamala Ray, Amalendu Banerjee, Dilip K. Bhattacharya
    Abstract:

    Diospyrin, a bisnaphthoquinonoid plant product and its derivatives have shown significant inhibitory activities against murine tumours in vivo. Studies on the haematological status, serum protein and creatinine levels, activities of several serum glycolytic enzymes, and histopathology of the mice inoculated with Ehrlich ascites carcinoma were carried out after treatment with Diospyrin and four synthetic derivatives. The prognostic significance of the pharmacological parameters acting as markers of the diseased state was evident from these findings. Normal mice were also studied before and after treatment with these compounds which did not cause noticeable adverse effects on the vital parameters, thereby indicating the possibility of the utilization of Diospyrin and derivatives as appropriate therapeutic agents.

  • in vitro antiplasmodial effects of Diospyrin a plant derived naphthoquinoid and a novel series of derivatives
    Phytotherapy Research, 1995
    Co-Authors: Banasri Hazra, Amalendu Banerjee, Rina Ghosh, G. C. Kirby, David C. Warhurst, David J Phillipson
    Abstract:

    Abstract Synthesis of derivatives of Diospyrin, a natural product, has led to the modification of its tumour-inhibitory effect, in vitro, towards Ehrlich ascites carcinoma and antiparasitic activity against Leishmania donovani in vitro. The present study shows that two of these novel hydroquinoid analogues derived from Diospyrin also show enhanced inhibitory effects against Plasmodium falciparum, in vitro, and may be a useful model for the development of novel antimalarial drugs.

  • In vitro antiplasmodial effects of Diospyrin, a plant‐derived naphthoquinoid, and a novel series of derivatives
    Phytotherapy Research, 1995
    Co-Authors: Banasri Hazra, Amalendu Banerjee, Rina Ghosh, G. C. Kirby, David C. Warhurst, J. David Phillipson
    Abstract:

    Abstract Synthesis of derivatives of Diospyrin, a natural product, has led to the modification of its tumour-inhibitory effect, in vitro, towards Ehrlich ascites carcinoma and antiparasitic activity against Leishmania donovani in vitro. The present study shows that two of these novel hydroquinoid analogues derived from Diospyrin also show enhanced inhibitory effects against Plasmodium falciparum, in vitro, and may be a useful model for the development of novel antimalarial drugs.

Rina Ghosh - One of the best experts on this subject based on the ideXlab platform.

  • Synthesis of novel aminoquinonoid analogues of Diospyrin and evaluation of their inhibitory activity against murine and human cancer cells.
    European journal of medicinal chemistry, 2007
    Co-Authors: Madhushree Das Sarma, Rina Ghosh, Amarendra Patra, Banasri Hazra
    Abstract:

    The synthesis and tumor-inhibitory activity of a series of aminonaphthoquinone derivatives of Diospyrin, which was isolated from Diospyros montana Roxb., are presented here for the first time. An aminoacetate derivative showed the maximum (approximately 93%) increase in life span in vivo against murine Ehrlich ascites carcinoma (EAC) at a dose of 1 mg kg(-1)day(-1) (ip; five doses), and the lowest IC50 (0.06 microM) in vitro. Further, the same analogue also exhibited considerable enhancement in antiproliferative activity when evaluated against human cell lines, viz. malignant skin melanoma and epidermoid laryngeal carcinoma (IC50=0.06 and 0.92 microM, respectively) in comparison to the natural precursor, Diospyrin (IC50=0.82 and 3.58 microM, respectively). Moreover, Diospyrin and all its derivatives were found to show significantly greater (approximately 17- to 1441-fold) cytotoxicity against the tumor cells as compared to normal human lymphocytes. All these quinonoids generated substantial amounts of reactive oxygen species in EAC cells, more or less commensurate to their respective IC50 values.

  • Novel glycoconjugates of Diospyrin, a quinonoid plant product: synthesis and evaluation of cytotoxicity against human malignant melanoma (A375) and laryngeal carcinoma (Hep2)
    Organic & biomolecular chemistry, 2007
    Co-Authors: Madhushree Das Sarma, Rina Ghosh, Amarendra Patra, Rajdeep Chowdhury, Keya Chaudhuri, Banasri Hazra
    Abstract:

    Glycoside derivatives of Diospyrin (1) were synthesized for the first time, and the cytotoxicity of the novel compounds vis-a-vis their precursors were evaluated against two human cancer cell lines, viz. malignant melanoma (A375) and laryngeal carcinoma (Hep2). The IC50 values were in the low micromolar range for all the compounds tested, and A375 cells showed comparatively greater sensitivity than Hep2. Most of the compounds exhibited enhanced activity as compared to the plant-derived quinonoid precursor of the series (1), while the aminophenyl mannosyl (6) was found to be the most effective derivative. In A375 cells, 6 (IC50 = 0.02 µM) showed the maximum increase in cytotoxicity (∼35-fold) over that of 1 (IC50 = 0.82 µM). Again, when the glycosides were evaluated at a given concentration (0.1 µM) for their relative capacity to generate ROS from A375 cells, the compound 6 could produce the highest amount of ROS. Incidentally, this derivative also showed a comparatively lower toxicity (IC50 ∼ 41 µM) when tested against normal human peripheral blood mononuclear cells, indicating a fair prospect of its development as a novel chemotherapeutic agent for the treatment of malignant melanoma.

  • Synthesis and antiproliferative activity of some novel derivatives of Diospyrin, a plant-derived naphthoquinonoid.
    Bioorganic & medicinal chemistry, 2007
    Co-Authors: Madhushree Das Sarma, Rina Ghosh, Amarendra Patra, Banasri Hazra
    Abstract:

    Derivatisation of Diospyrin, a bisnaphthoquinonoid isolated from Diospyros montana Roxb., led to the modification of its inhibitory activity, in vitro, towards a murine tumour model, Ehrlich ascites carcinoma (EAC), and two human cancer cell lines, viz., malignant skin melanoma (A375) and epidermoid laryngeal carcinoma (Hep2). Among the novel derivatives, an epoxide exhibited the maximum antiproliferative activity (IC(50) values in the range of 0.03-0.21 microM) and a comparatively lower toxicity (IC(50) approximately 98 microM) in normal human peripheral blood mononuclear cells (PBMC). This compound might provide a novel 'lead' for the development of clinically effective antiproliferative agents against cancer.

  • WITHDRAWN: Novel aminoquinonoid analogues of Diospyrin: Synthesis, antitumour activity and preliminary QSAR studies
    Bioorganic & medicinal chemistry, 2006
    Co-Authors: Madhushree Das Sarma, Rina Ghosh, Amarendra Patra, Pooja Sharma, Nanda Ghoshal, Banasri Hazra
    Abstract:

    This article has been retracted, consistent with Elsevier Policy on Article Withdrawal. Please see http://www.elsevier.com/locate/withdrawalpolicy. The Publisher apologizes for any inconvenience this may cause.

  • in vitro antiplasmodial effects of Diospyrin a plant derived naphthoquinoid and a novel series of derivatives
    Phytotherapy Research, 1995
    Co-Authors: Banasri Hazra, Amalendu Banerjee, Rina Ghosh, G. C. Kirby, David C. Warhurst, David J Phillipson
    Abstract:

    Abstract Synthesis of derivatives of Diospyrin, a natural product, has led to the modification of its tumour-inhibitory effect, in vitro, towards Ehrlich ascites carcinoma and antiparasitic activity against Leishmania donovani in vitro. The present study shows that two of these novel hydroquinoid analogues derived from Diospyrin also show enhanced inhibitory effects against Plasmodium falciparum, in vitro, and may be a useful model for the development of novel antimalarial drugs.

Dilip K. Bhattacharya - One of the best experts on this subject based on the ideXlab platform.

  • pharmacological studies on the effect of the treatment of swiss a mice with Diospyrin a tumour inhibitory plant product and its synthetic derivatives
    Phytotherapy Research, 1996
    Co-Authors: Sampa Pal, Banasri Hazra, Ratnamala Ray, Amalendu Banerjee, Dilip K. Bhattacharya
    Abstract:

    Diospyrin, a bisnaphthoquinonoid plant product and its derivatives have shown significant inhibitory activities against murine tumours in vivo. Studies on the haematological status, serum protein and creatinine levels, activities of several serum glycolytic enzymes, and histopathology of the mice inoculated with Ehrlich ascites carcinoma were carried out after treatment with Diospyrin and four synthetic derivatives. The prognostic significance of the pharmacological parameters acting as markers of the diseased state was evident from these findings. Normal mice were also studied before and after treatment with these compounds which did not cause noticeable adverse effects on the vital parameters, thereby indicating the possibility of the utilization of Diospyrin and derivatives as appropriate therapeutic agents.

  • Pharmacological Studies on the Effect of the Treatment of Swiss A Mice with Diospyrin, a Tumour‐inhibitory Plant Product, and its Synthetic Derivatives
    Phytotherapy Research, 1996
    Co-Authors: Sampa Pal, Banasri Hazra, Ratnamala Ray, Amalendu Banerjee, Dilip K. Bhattacharya
    Abstract:

    Diospyrin, a bisnaphthoquinonoid plant product and its derivatives have shown significant inhibitory activities against murine tumours in vivo. Studies on the haematological status, serum protein and creatinine levels, activities of several serum glycolytic enzymes, and histopathology of the mice inoculated with Ehrlich ascites carcinoma were carried out after treatment with Diospyrin and four synthetic derivatives. The prognostic significance of the pharmacological parameters acting as markers of the diseased state was evident from these findings. Normal mice were also studied before and after treatment with these compounds which did not cause noticeable adverse effects on the vital parameters, thereby indicating the possibility of the utilization of Diospyrin and derivatives as appropriate therapeutic agents.

Madhushree Das Sarma - One of the best experts on this subject based on the ideXlab platform.

  • Evaluation of a Diospyrin derivative as antileishmanial agent and potential modulator of ornithine decarboxylase of Leishmania donovani
    Experimental parasitology, 2013
    Co-Authors: Sudipta Hazra, Madhushree Das Sarma, Subhalakshmi Ghosh, Smriti Sharma, Mousumi Das, Prakash Saudagar, Vijay Kumar Prajapati, Vikash Kumar Dubey, Shyam Sundar, Banasri Hazra
    Abstract:

    Abstract World health organization has called for academic research and development of new chemotherapeutic strategies to overcome the emerging resistance and side effects exhibited by the drugs currently used against leishmaniasis. Diospyrin, a bis-naphthoquinone isolated from Diospyros montana Roxb., and its semi-synthetic derivatives, were reported for inhibitory activity against protozoan parasites including Leishmania. Presently, we have investigated the antileishmanial effect of a di-epoxide derivative of Diospyrin (D17), both in vitro and in vivo. Further, the safety profile of D17 was established by testing its toxicity against normal macrophage cells (IC50 ∼ 20.7 μM), and also against normal BALB/c mice in vivo. The compound showed enhanced activity (IC50 ∼ 7.2 μM) as compared to Diospyrin (IC50 ∼ 12.6 μM) against Leishmania donovani promastigotes. Again, D17 was tested on L. donovani BHU1216 isolated from a sodium stibogluconate-unresponsive patient, and exhibited selective inhibition of the intracellular amastigotes (IC50 ∼ 0.18 μM). Also, treatment of infected BALB/c mice with D17 at 2 mg/kg/day reduced the hepatic parasite load by about 38%. Subsequently, computational docking studies were undertaken on selected enzymes of trypanothione metabolism, viz. trypanothione reductase (TryR) and ornithine decarboxylase (ODC), followed by the enzyme kinetics, where D17 demonstrated non-competitive inhibition of the L. donovani ODC, but could not inhibit TryR.

  • Synthesis of novel aminoquinonoid analogues of Diospyrin and evaluation of their inhibitory activity against murine and human cancer cells.
    European journal of medicinal chemistry, 2007
    Co-Authors: Madhushree Das Sarma, Rina Ghosh, Amarendra Patra, Banasri Hazra
    Abstract:

    The synthesis and tumor-inhibitory activity of a series of aminonaphthoquinone derivatives of Diospyrin, which was isolated from Diospyros montana Roxb., are presented here for the first time. An aminoacetate derivative showed the maximum (approximately 93%) increase in life span in vivo against murine Ehrlich ascites carcinoma (EAC) at a dose of 1 mg kg(-1)day(-1) (ip; five doses), and the lowest IC50 (0.06 microM) in vitro. Further, the same analogue also exhibited considerable enhancement in antiproliferative activity when evaluated against human cell lines, viz. malignant skin melanoma and epidermoid laryngeal carcinoma (IC50=0.06 and 0.92 microM, respectively) in comparison to the natural precursor, Diospyrin (IC50=0.82 and 3.58 microM, respectively). Moreover, Diospyrin and all its derivatives were found to show significantly greater (approximately 17- to 1441-fold) cytotoxicity against the tumor cells as compared to normal human lymphocytes. All these quinonoids generated substantial amounts of reactive oxygen species in EAC cells, more or less commensurate to their respective IC50 values.

  • Novel glycoconjugates of Diospyrin, a quinonoid plant product: synthesis and evaluation of cytotoxicity against human malignant melanoma (A375) and laryngeal carcinoma (Hep2)
    Organic & biomolecular chemistry, 2007
    Co-Authors: Madhushree Das Sarma, Rina Ghosh, Amarendra Patra, Rajdeep Chowdhury, Keya Chaudhuri, Banasri Hazra
    Abstract:

    Glycoside derivatives of Diospyrin (1) were synthesized for the first time, and the cytotoxicity of the novel compounds vis-a-vis their precursors were evaluated against two human cancer cell lines, viz. malignant melanoma (A375) and laryngeal carcinoma (Hep2). The IC50 values were in the low micromolar range for all the compounds tested, and A375 cells showed comparatively greater sensitivity than Hep2. Most of the compounds exhibited enhanced activity as compared to the plant-derived quinonoid precursor of the series (1), while the aminophenyl mannosyl (6) was found to be the most effective derivative. In A375 cells, 6 (IC50 = 0.02 µM) showed the maximum increase in cytotoxicity (∼35-fold) over that of 1 (IC50 = 0.82 µM). Again, when the glycosides were evaluated at a given concentration (0.1 µM) for their relative capacity to generate ROS from A375 cells, the compound 6 could produce the highest amount of ROS. Incidentally, this derivative also showed a comparatively lower toxicity (IC50 ∼ 41 µM) when tested against normal human peripheral blood mononuclear cells, indicating a fair prospect of its development as a novel chemotherapeutic agent for the treatment of malignant melanoma.

  • Synthesis and antiproliferative activity of some novel derivatives of Diospyrin, a plant-derived naphthoquinonoid.
    Bioorganic & medicinal chemistry, 2007
    Co-Authors: Madhushree Das Sarma, Rina Ghosh, Amarendra Patra, Banasri Hazra
    Abstract:

    Derivatisation of Diospyrin, a bisnaphthoquinonoid isolated from Diospyros montana Roxb., led to the modification of its inhibitory activity, in vitro, towards a murine tumour model, Ehrlich ascites carcinoma (EAC), and two human cancer cell lines, viz., malignant skin melanoma (A375) and epidermoid laryngeal carcinoma (Hep2). Among the novel derivatives, an epoxide exhibited the maximum antiproliferative activity (IC(50) values in the range of 0.03-0.21 microM) and a comparatively lower toxicity (IC(50) approximately 98 microM) in normal human peripheral blood mononuclear cells (PBMC). This compound might provide a novel 'lead' for the development of clinically effective antiproliferative agents against cancer.

  • WITHDRAWN: Novel aminoquinonoid analogues of Diospyrin: Synthesis, antitumour activity and preliminary QSAR studies
    Bioorganic & medicinal chemistry, 2006
    Co-Authors: Madhushree Das Sarma, Rina Ghosh, Amarendra Patra, Pooja Sharma, Nanda Ghoshal, Banasri Hazra
    Abstract:

    This article has been retracted, consistent with Elsevier Policy on Article Withdrawal. Please see http://www.elsevier.com/locate/withdrawalpolicy. The Publisher apologizes for any inconvenience this may cause.