The Experts below are selected from a list of 228 Experts worldwide ranked by ideXlab platform
Runtao Li - One of the best experts on this subject based on the ideXlab platform.
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novel Dithiocarbamic Acid esters derived from 6 aminomethyl 4 anilinoquinazolines and 6 aminomethyl 4 anilino 3 cyanoquinolines as potent egfr inhibitors
Archiv Der Pharmazie, 2013Co-Authors: Xin Zhang, Ridong Li, Kang Qiao, Zemei Ge, Liangren Zhang, Tieming Cheng, Runtao LiAbstract:Two series of Dithiocarbamic Acid esters, 4-anilinoquinazoline-6-ylmethylcarbamodithioic Acid esters and 3-cyano-4-anilinoquinolin-6-ylmethylcarbamodithioic Acid esters, were designed and synthesized. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay against three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Most of the compounds are equally or more potent than the positive control lapatinib. Three compounds (14d, 14h and 14i) were identified as dual inhibitors of the EGFR and ErbB-2 kinases and two compounds (14b and 14c) were identified as multi-target kinase inhibitors, and they are very worthy of further study. Installation of the Dithiocarbamic Acid ester group at the 6-position of 4-anilinoquinazoline or 3-cyano-4-anilinoquinoline could improve the inhibitory activity. Different Dithiocarbamic Acid ester groups significantly affect the activities.
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Novel Dithiocarbamic Acid Esters Derived from 6‐Aminomethyl‐4‐anilinoquinazolines and 6‐Aminomethyl‐4‐anilino‐3‐cyanoquinolines as Potent EGFR Inhibitors
Archiv Der Pharmazie, 2012Co-Authors: Xin Zhang, Ridong Li, Kang Qiao, Zemei Ge, Liangren Zhang, Tieming Cheng, Runtao LiAbstract:Two series of Dithiocarbamic Acid esters, 4-anilinoquinazoline-6-ylmethylcarbamodithioic Acid esters and 3-cyano-4-anilinoquinolin-6-ylmethylcarbamodithioic Acid esters, were designed and synthesized. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay against three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Most of the compounds are equally or more potent than the positive control lapatinib. Three compounds (14d, 14h and 14i) were identified as dual inhibitors of the EGFR and ErbB-2 kinases and two compounds (14b and 14c) were identified as multi-target kinase inhibitors, and they are very worthy of further study. Installation of the Dithiocarbamic Acid ester group at the 6-position of 4-anilinoquinazoline or 3-cyano-4-anilinoquinoline could improve the inhibitory activity. Different Dithiocarbamic Acid ester groups significantly affect the activities.
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novel egfr inhibitors prepared by combination of Dithiocarbamic Acid esters and 4 anilinoquinazolines
Bioorganic & Medicinal Chemistry Letters, 2011Co-Authors: Ridong Li, Xin Zhang, Zemei Ge, Qiaoyan Li, Runtao LiAbstract:On the basis of combination strategy, a novel series of EGFR inhibitors were designed and synthesized by combination of Dithiocarbamic Acid esters and 4-anilinoquinazolines. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay in three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Two compounds (11d and 11f) were found more potent against all three cell lines and five compounds (11a, 11d-11g) were found more potent against both MDA-MB-468 and SK-BR-3 than Lapatinib. SAR studies revealed that the substituents on C6 and C7 positions of quinazoline, the amine component of dithiocarbamate moiety and the linker greatly affected the activity. This work provides a promising new strategy for the preparation of potent tyrosine kinase inhibitors.
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synthesis and structure activity relationships of a novel class of Dithiocarbamic Acid esters as anticancer agent
Archiv Der Pharmazie, 2011Co-Authors: Zemei Ge, Tingmin Wang, Jun Wu, Runtao LiAbstract:Based on a novel lead compound 4-methylpiperazine-1-carbodithioic Acid 3-cyano-3,3-diphenylpropyl ester 1, the systematic structural modification was carried out. All the synthesized compounds were evaluated for their in-vitro anticancer activities on four to six different cell lines at three different concentrations. Most of the tested compounds could selectively inhibit the growth of HL-60 and Bel-7402 cell lines at a medium concentration. Four compounds (3f, 3g, 3n, and 5) were selected for the IC(50) test, and the results revealed that three compounds (3g, 3n, and 5) showed almost the same or a slightly weaker activity than compound 1 against HL-60, and three compounds (3f, 3g, and 3n) showed > 2-fold higher potency than compound 1 against Bel-7402. The in-vivo efficacy of 3n center dot HCl was evaluated with transplanted hepatocyte carcinoma 22 as an in-vivo test model. It was found that 3n center dot HCl could inhibit significantly the growth of tumor, and that this effect was dose-dependent. Meanwhile, the compound 3n center dot HCl showed low toxicity compared with compound 1 center dot HCl as evidenced by the little body-weight loss. These results confirmed that compound 3n center dot HCl is more potent than the lead compound 1 center dot HCl. Preliminary structure-activity relationships indicated that: a) Both nitrile group and the cyclic amine containing at least two nitrogens were indispensable moieties to keep the activity; b) substitution of the piperazine ring is unfavorable for the improvement of activity; c) the suitable linker joining the piperazinyl dithiocarboxyl and diphenylacetonitril group should be ethylene; d) a non-coplanar arrangement of the two benzene rings appears to be essential for activity.
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Dithiocarbamic Acid esters as anticancer agent part 1 4 substituted piperazine 1 carbodithioic Acid 3 cyano 3 3 diphenyl propyl esters
Bioorganic & Medicinal Chemistry Letters, 2006Co-Authors: Zemei Ge, Tieming Cheng, Tingmin Wang, Runtao LiAbstract:Abstract A variety of 4-N atom substituted derivatives were synthesized and evaluated for their in vitro anticancer activities using 4-methylpiperazine-1-carbodithioic Acid 3-cyano-3,3-diphenyl-propyl ester 4 as lead compound. Among them, compound 6a without any substituent on 4-N atom (R 1 = H) was found to be the most active anticancer agent with IC 50 = 5.3 μM against HL-60 and IC 50 = 11.5 μM against Bel-7402, respectively. Increase in the polarity and/or introduction of suitable acyl groups at the 4-N atom of the lead compound 4 are favorable for the improvement of activity.
Zemei Ge - One of the best experts on this subject based on the ideXlab platform.
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novel Dithiocarbamic Acid esters derived from 6 aminomethyl 4 anilinoquinazolines and 6 aminomethyl 4 anilino 3 cyanoquinolines as potent egfr inhibitors
Archiv Der Pharmazie, 2013Co-Authors: Xin Zhang, Ridong Li, Kang Qiao, Zemei Ge, Liangren Zhang, Tieming Cheng, Runtao LiAbstract:Two series of Dithiocarbamic Acid esters, 4-anilinoquinazoline-6-ylmethylcarbamodithioic Acid esters and 3-cyano-4-anilinoquinolin-6-ylmethylcarbamodithioic Acid esters, were designed and synthesized. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay against three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Most of the compounds are equally or more potent than the positive control lapatinib. Three compounds (14d, 14h and 14i) were identified as dual inhibitors of the EGFR and ErbB-2 kinases and two compounds (14b and 14c) were identified as multi-target kinase inhibitors, and they are very worthy of further study. Installation of the Dithiocarbamic Acid ester group at the 6-position of 4-anilinoquinazoline or 3-cyano-4-anilinoquinoline could improve the inhibitory activity. Different Dithiocarbamic Acid ester groups significantly affect the activities.
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Novel Dithiocarbamic Acid Esters Derived from 6‐Aminomethyl‐4‐anilinoquinazolines and 6‐Aminomethyl‐4‐anilino‐3‐cyanoquinolines as Potent EGFR Inhibitors
Archiv Der Pharmazie, 2012Co-Authors: Xin Zhang, Ridong Li, Kang Qiao, Zemei Ge, Liangren Zhang, Tieming Cheng, Runtao LiAbstract:Two series of Dithiocarbamic Acid esters, 4-anilinoquinazoline-6-ylmethylcarbamodithioic Acid esters and 3-cyano-4-anilinoquinolin-6-ylmethylcarbamodithioic Acid esters, were designed and synthesized. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay against three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Most of the compounds are equally or more potent than the positive control lapatinib. Three compounds (14d, 14h and 14i) were identified as dual inhibitors of the EGFR and ErbB-2 kinases and two compounds (14b and 14c) were identified as multi-target kinase inhibitors, and they are very worthy of further study. Installation of the Dithiocarbamic Acid ester group at the 6-position of 4-anilinoquinazoline or 3-cyano-4-anilinoquinoline could improve the inhibitory activity. Different Dithiocarbamic Acid ester groups significantly affect the activities.
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novel egfr inhibitors prepared by combination of Dithiocarbamic Acid esters and 4 anilinoquinazolines
Bioorganic & Medicinal Chemistry Letters, 2011Co-Authors: Ridong Li, Xin Zhang, Zemei Ge, Qiaoyan Li, Runtao LiAbstract:On the basis of combination strategy, a novel series of EGFR inhibitors were designed and synthesized by combination of Dithiocarbamic Acid esters and 4-anilinoquinazolines. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay in three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Two compounds (11d and 11f) were found more potent against all three cell lines and five compounds (11a, 11d-11g) were found more potent against both MDA-MB-468 and SK-BR-3 than Lapatinib. SAR studies revealed that the substituents on C6 and C7 positions of quinazoline, the amine component of dithiocarbamate moiety and the linker greatly affected the activity. This work provides a promising new strategy for the preparation of potent tyrosine kinase inhibitors.
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synthesis and structure activity relationships of a novel class of Dithiocarbamic Acid esters as anticancer agent
Archiv Der Pharmazie, 2011Co-Authors: Zemei Ge, Tingmin Wang, Jun Wu, Runtao LiAbstract:Based on a novel lead compound 4-methylpiperazine-1-carbodithioic Acid 3-cyano-3,3-diphenylpropyl ester 1, the systematic structural modification was carried out. All the synthesized compounds were evaluated for their in-vitro anticancer activities on four to six different cell lines at three different concentrations. Most of the tested compounds could selectively inhibit the growth of HL-60 and Bel-7402 cell lines at a medium concentration. Four compounds (3f, 3g, 3n, and 5) were selected for the IC(50) test, and the results revealed that three compounds (3g, 3n, and 5) showed almost the same or a slightly weaker activity than compound 1 against HL-60, and three compounds (3f, 3g, and 3n) showed > 2-fold higher potency than compound 1 against Bel-7402. The in-vivo efficacy of 3n center dot HCl was evaluated with transplanted hepatocyte carcinoma 22 as an in-vivo test model. It was found that 3n center dot HCl could inhibit significantly the growth of tumor, and that this effect was dose-dependent. Meanwhile, the compound 3n center dot HCl showed low toxicity compared with compound 1 center dot HCl as evidenced by the little body-weight loss. These results confirmed that compound 3n center dot HCl is more potent than the lead compound 1 center dot HCl. Preliminary structure-activity relationships indicated that: a) Both nitrile group and the cyclic amine containing at least two nitrogens were indispensable moieties to keep the activity; b) substitution of the piperazine ring is unfavorable for the improvement of activity; c) the suitable linker joining the piperazinyl dithiocarboxyl and diphenylacetonitril group should be ethylene; d) a non-coplanar arrangement of the two benzene rings appears to be essential for activity.
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Dithiocarbamic Acid esters as anticancer agent part 1 4 substituted piperazine 1 carbodithioic Acid 3 cyano 3 3 diphenyl propyl esters
Bioorganic & Medicinal Chemistry Letters, 2006Co-Authors: Zemei Ge, Tieming Cheng, Tingmin Wang, Runtao LiAbstract:Abstract A variety of 4-N atom substituted derivatives were synthesized and evaluated for their in vitro anticancer activities using 4-methylpiperazine-1-carbodithioic Acid 3-cyano-3,3-diphenyl-propyl ester 4 as lead compound. Among them, compound 6a without any substituent on 4-N atom (R 1 = H) was found to be the most active anticancer agent with IC 50 = 5.3 μM against HL-60 and IC 50 = 11.5 μM against Bel-7402, respectively. Increase in the polarity and/or introduction of suitable acyl groups at the 4-N atom of the lead compound 4 are favorable for the improvement of activity.
Ridong Li - One of the best experts on this subject based on the ideXlab platform.
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novel Dithiocarbamic Acid esters derived from 6 aminomethyl 4 anilinoquinazolines and 6 aminomethyl 4 anilino 3 cyanoquinolines as potent egfr inhibitors
Archiv Der Pharmazie, 2013Co-Authors: Xin Zhang, Ridong Li, Kang Qiao, Zemei Ge, Liangren Zhang, Tieming Cheng, Runtao LiAbstract:Two series of Dithiocarbamic Acid esters, 4-anilinoquinazoline-6-ylmethylcarbamodithioic Acid esters and 3-cyano-4-anilinoquinolin-6-ylmethylcarbamodithioic Acid esters, were designed and synthesized. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay against three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Most of the compounds are equally or more potent than the positive control lapatinib. Three compounds (14d, 14h and 14i) were identified as dual inhibitors of the EGFR and ErbB-2 kinases and two compounds (14b and 14c) were identified as multi-target kinase inhibitors, and they are very worthy of further study. Installation of the Dithiocarbamic Acid ester group at the 6-position of 4-anilinoquinazoline or 3-cyano-4-anilinoquinoline could improve the inhibitory activity. Different Dithiocarbamic Acid ester groups significantly affect the activities.
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Novel Dithiocarbamic Acid Esters Derived from 6‐Aminomethyl‐4‐anilinoquinazolines and 6‐Aminomethyl‐4‐anilino‐3‐cyanoquinolines as Potent EGFR Inhibitors
Archiv Der Pharmazie, 2012Co-Authors: Xin Zhang, Ridong Li, Kang Qiao, Zemei Ge, Liangren Zhang, Tieming Cheng, Runtao LiAbstract:Two series of Dithiocarbamic Acid esters, 4-anilinoquinazoline-6-ylmethylcarbamodithioic Acid esters and 3-cyano-4-anilinoquinolin-6-ylmethylcarbamodithioic Acid esters, were designed and synthesized. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay against three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Most of the compounds are equally or more potent than the positive control lapatinib. Three compounds (14d, 14h and 14i) were identified as dual inhibitors of the EGFR and ErbB-2 kinases and two compounds (14b and 14c) were identified as multi-target kinase inhibitors, and they are very worthy of further study. Installation of the Dithiocarbamic Acid ester group at the 6-position of 4-anilinoquinazoline or 3-cyano-4-anilinoquinoline could improve the inhibitory activity. Different Dithiocarbamic Acid ester groups significantly affect the activities.
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novel egfr inhibitors prepared by combination of Dithiocarbamic Acid esters and 4 anilinoquinazolines
Bioorganic & Medicinal Chemistry Letters, 2011Co-Authors: Ridong Li, Xin Zhang, Zemei Ge, Qiaoyan Li, Runtao LiAbstract:On the basis of combination strategy, a novel series of EGFR inhibitors were designed and synthesized by combination of Dithiocarbamic Acid esters and 4-anilinoquinazolines. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay in three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Two compounds (11d and 11f) were found more potent against all three cell lines and five compounds (11a, 11d-11g) were found more potent against both MDA-MB-468 and SK-BR-3 than Lapatinib. SAR studies revealed that the substituents on C6 and C7 positions of quinazoline, the amine component of dithiocarbamate moiety and the linker greatly affected the activity. This work provides a promising new strategy for the preparation of potent tyrosine kinase inhibitors.
Xin Zhang - One of the best experts on this subject based on the ideXlab platform.
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novel Dithiocarbamic Acid esters derived from 6 aminomethyl 4 anilinoquinazolines and 6 aminomethyl 4 anilino 3 cyanoquinolines as potent egfr inhibitors
Archiv Der Pharmazie, 2013Co-Authors: Xin Zhang, Ridong Li, Kang Qiao, Zemei Ge, Liangren Zhang, Tieming Cheng, Runtao LiAbstract:Two series of Dithiocarbamic Acid esters, 4-anilinoquinazoline-6-ylmethylcarbamodithioic Acid esters and 3-cyano-4-anilinoquinolin-6-ylmethylcarbamodithioic Acid esters, were designed and synthesized. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay against three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Most of the compounds are equally or more potent than the positive control lapatinib. Three compounds (14d, 14h and 14i) were identified as dual inhibitors of the EGFR and ErbB-2 kinases and two compounds (14b and 14c) were identified as multi-target kinase inhibitors, and they are very worthy of further study. Installation of the Dithiocarbamic Acid ester group at the 6-position of 4-anilinoquinazoline or 3-cyano-4-anilinoquinoline could improve the inhibitory activity. Different Dithiocarbamic Acid ester groups significantly affect the activities.
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Novel Dithiocarbamic Acid Esters Derived from 6‐Aminomethyl‐4‐anilinoquinazolines and 6‐Aminomethyl‐4‐anilino‐3‐cyanoquinolines as Potent EGFR Inhibitors
Archiv Der Pharmazie, 2012Co-Authors: Xin Zhang, Ridong Li, Kang Qiao, Zemei Ge, Liangren Zhang, Tieming Cheng, Runtao LiAbstract:Two series of Dithiocarbamic Acid esters, 4-anilinoquinazoline-6-ylmethylcarbamodithioic Acid esters and 3-cyano-4-anilinoquinolin-6-ylmethylcarbamodithioic Acid esters, were designed and synthesized. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay against three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Most of the compounds are equally or more potent than the positive control lapatinib. Three compounds (14d, 14h and 14i) were identified as dual inhibitors of the EGFR and ErbB-2 kinases and two compounds (14b and 14c) were identified as multi-target kinase inhibitors, and they are very worthy of further study. Installation of the Dithiocarbamic Acid ester group at the 6-position of 4-anilinoquinazoline or 3-cyano-4-anilinoquinoline could improve the inhibitory activity. Different Dithiocarbamic Acid ester groups significantly affect the activities.
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novel egfr inhibitors prepared by combination of Dithiocarbamic Acid esters and 4 anilinoquinazolines
Bioorganic & Medicinal Chemistry Letters, 2011Co-Authors: Ridong Li, Xin Zhang, Zemei Ge, Qiaoyan Li, Runtao LiAbstract:On the basis of combination strategy, a novel series of EGFR inhibitors were designed and synthesized by combination of Dithiocarbamic Acid esters and 4-anilinoquinazolines. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay in three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Two compounds (11d and 11f) were found more potent against all three cell lines and five compounds (11a, 11d-11g) were found more potent against both MDA-MB-468 and SK-BR-3 than Lapatinib. SAR studies revealed that the substituents on C6 and C7 positions of quinazoline, the amine component of dithiocarbamate moiety and the linker greatly affected the activity. This work provides a promising new strategy for the preparation of potent tyrosine kinase inhibitors.
Tieming Cheng - One of the best experts on this subject based on the ideXlab platform.
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novel Dithiocarbamic Acid esters derived from 6 aminomethyl 4 anilinoquinazolines and 6 aminomethyl 4 anilino 3 cyanoquinolines as potent egfr inhibitors
Archiv Der Pharmazie, 2013Co-Authors: Xin Zhang, Ridong Li, Kang Qiao, Zemei Ge, Liangren Zhang, Tieming Cheng, Runtao LiAbstract:Two series of Dithiocarbamic Acid esters, 4-anilinoquinazoline-6-ylmethylcarbamodithioic Acid esters and 3-cyano-4-anilinoquinolin-6-ylmethylcarbamodithioic Acid esters, were designed and synthesized. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay against three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Most of the compounds are equally or more potent than the positive control lapatinib. Three compounds (14d, 14h and 14i) were identified as dual inhibitors of the EGFR and ErbB-2 kinases and two compounds (14b and 14c) were identified as multi-target kinase inhibitors, and they are very worthy of further study. Installation of the Dithiocarbamic Acid ester group at the 6-position of 4-anilinoquinazoline or 3-cyano-4-anilinoquinoline could improve the inhibitory activity. Different Dithiocarbamic Acid ester groups significantly affect the activities.
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Novel Dithiocarbamic Acid Esters Derived from 6‐Aminomethyl‐4‐anilinoquinazolines and 6‐Aminomethyl‐4‐anilino‐3‐cyanoquinolines as Potent EGFR Inhibitors
Archiv Der Pharmazie, 2012Co-Authors: Xin Zhang, Ridong Li, Kang Qiao, Zemei Ge, Liangren Zhang, Tieming Cheng, Runtao LiAbstract:Two series of Dithiocarbamic Acid esters, 4-anilinoquinazoline-6-ylmethylcarbamodithioic Acid esters and 3-cyano-4-anilinoquinolin-6-ylmethylcarbamodithioic Acid esters, were designed and synthesized. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay against three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Most of the compounds are equally or more potent than the positive control lapatinib. Three compounds (14d, 14h and 14i) were identified as dual inhibitors of the EGFR and ErbB-2 kinases and two compounds (14b and 14c) were identified as multi-target kinase inhibitors, and they are very worthy of further study. Installation of the Dithiocarbamic Acid ester group at the 6-position of 4-anilinoquinazoline or 3-cyano-4-anilinoquinoline could improve the inhibitory activity. Different Dithiocarbamic Acid ester groups significantly affect the activities.
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Dithiocarbamic Acid esters as anticancer agent part 1 4 substituted piperazine 1 carbodithioic Acid 3 cyano 3 3 diphenyl propyl esters
Bioorganic & Medicinal Chemistry Letters, 2006Co-Authors: Zemei Ge, Tieming Cheng, Tingmin Wang, Runtao LiAbstract:Abstract A variety of 4-N atom substituted derivatives were synthesized and evaluated for their in vitro anticancer activities using 4-methylpiperazine-1-carbodithioic Acid 3-cyano-3,3-diphenyl-propyl ester 4 as lead compound. Among them, compound 6a without any substituent on 4-N atom (R 1 = H) was found to be the most active anticancer agent with IC 50 = 5.3 μM against HL-60 and IC 50 = 11.5 μM against Bel-7402, respectively. Increase in the polarity and/or introduction of suitable acyl groups at the 4-N atom of the lead compound 4 are favorable for the improvement of activity.