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Antineoplastic Activity

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Michael P. Vezeridis – One of the best experts on this subject based on the ideXlab platform.

  • Antineoplastic Activity of a rhodium trichloride complex of oxalyl homocysteine thiolactone.
    Cancer Investigation, 2009
    Co-Authors: Kilmer S. Mccully, Michael P. Vezeridis

    Abstract:

    AbstractIn malignant cells the amino groups of cellular proteins are alkylated by homocysteine thiolactone, forming homocysteinyl peptide bonds. In nonnal cells the sulfur atom of homocysteine thiolactone is converted to homocysteic acid, phosphoadenosine phosphosulfate, and sulfate ester. N-substituted derivatives of homocysteine thiolactone synthesized from arachidonic acid, pyridoxal, and maleimide were previously found to have Antineoplastic Activity. Another N-substituted derivative, the rhodium trichloride complex of oxalyl homocysteine thiolactone, was synthesized and tested for Antineoplastic Activity. Mice with transplanted rhabdomyosarcoma were injected with solutions of the complex dissolved in lipids. Doses of 50 and 100 mg/kg per day for two weeks produced 50% inhibition of tumor growth. At doses of 100 and 200 mg/kg per day in tumor-free inice there was decreased survival, peritoneal reaction, pigment deposition in lung, jibrocalcijc pericarditis, and leiomyosarcoma of colon (in one animal)….

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Kilmer S. Mccully – One of the best experts on this subject based on the ideXlab platform.

  • Antineoplastic Activity of a rhodium trichloride complex of oxalyl homocysteine thiolactone.
    Cancer Investigation, 2009
    Co-Authors: Kilmer S. Mccully, Michael P. Vezeridis

    Abstract:

    AbstractIn malignant cells the amino groups of cellular proteins are alkylated by homocysteine thiolactone, forming homocysteinyl peptide bonds. In nonnal cells the sulfur atom of homocysteine thiolactone is converted to homocysteic acid, phosphoadenosine phosphosulfate, and sulfate ester. N-substituted derivatives of homocysteine thiolactone synthesized from arachidonic acid, pyridoxal, and maleimide were previously found to have Antineoplastic Activity. Another N-substituted derivative, the rhodium trichloride complex of oxalyl homocysteine thiolactone, was synthesized and tested for Antineoplastic Activity. Mice with transplanted rhabdomyosarcoma were injected with solutions of the complex dissolved in lipids. Doses of 50 and 100 mg/kg per day for two weeks produced 50% inhibition of tumor growth. At doses of 100 and 200 mg/kg per day in tumor-free inice there was decreased survival, peritoneal reaction, pigment deposition in lung, jibrocalcijc pericarditis, and leiomyosarcoma of colon (in one animal)….

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Dharam Paul Jindal – One of the best experts on this subject based on the ideXlab platform.

  • Synthesis and Antineoplastic Activity of some 16- benzylidene substituted steroidal oximes
    Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry, 2005
    Co-Authors: Sonal Dubey, Dharam Paul Jindal, Poonam Piplani

    Abstract:

    Novel 16-benzylidine substituted steroidal oximes in the androstene series have been designed, synthesized and evaluated for in vitro Antineoplastic Activity at NCI, Bethesda, USA against 3-cell lines using one dose primary anticancer assay. Of the compounds tested, 3β-hydroxy derivatives 24 (DPJ-1059), 26 (DPJ-1081), 28 (DPJ-870). 30 (DPJ-818), 32 (DPJ-854) and 3β-aceloxy derivatives 25 (DPJ-1061), 27 (DPJ-1083), 31 (DPJ-817) and 33(DPJ-900) have been found to be quite active.

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  • Synthesis and Antineoplastic Activity of 2-alkylaminoethyl derivatives of various steroidal oximes.
    European journal of medicinal chemistry, 2003
    Co-Authors: Dharam Paul Jindal, Sheetal Guleria, Raja Chattopadhaya, Ranju Gupta

    Abstract:

    Various steroidal oxime ether derivatives in androstene and estrane series have been synthesized and evaluated for the Antineoplastic Activity at National Cancer Institute, Bethesda, Maryland, USA. O-alkylation of the oximes by various alkylaminoethyl halides gave the oxime ether derivatives. The 17alpha-ethynylandrostene derivatives 29 (DPJ-684), 30 (DPJ-685), 31 (DPJ-686) and estrane derivatives 35 (DPJ-531) and 36 (DPJ-532) were among the small percentage of compounds, which have been screened by NCI for in vivo hollow fiber assay by virtue of their Activity against one or more human tumour cell lines in 60 cell line in vitro prescreen. The preliminary in vivo reports of hollow fiber assays have been referred to the Biological Evaluation Committee for Cancer Drugs for considering these compounds for further detailed in vivo testing.

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