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Your search keyword '"Rama K. Narla"' showing total 3 results
Start Over Author "Rama K. Narla" Journal bioorganic & medicinal chemistry letters
3 results on '"Rama K. Narla"'

1. A rationally designed anticancer drug targeting a unique binding cavity of tubulin

Author

Fatih M. Uckun, Christopher S. Navara, Alexei O. Vassilev, Rama K. Narla, Shyi Tai Jan, and Chen Mao

Subjects
Models, Molecular, Protein Conformation, Clinical Biochemistry, Pharmaceutical Science, Antineoplastic Agents, Tumor cells, Pharmacology, Biochemistry, Protein structure, Tubulin, Drug Discovery, Tumor Cells, Cultured, Humans, Furans, Molecular Biology, biology, Chemistry, Organic Chemistry, Biological activity, Anticancer drug, Drug Design, biology.protein, Molecular Medicine, Drug Screening Assays, Antitumor, Fatty Alcohols
Abstract

A novel mono-THF containing synthetic anticancer drug (WHI-261) was designed for targeting a previously unrecognized unique narrow binding cavity on the surface of tubulin. The anti-cancer activity of WHI-261 was confirmed using MTT assays. The structure-based design, synthesis, and biological activity of WHI-261 are reported.

Published
2000
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2. Organic phenyl arsonic acid compounds with potent antileukemic activity

Author

Xing-Ping Liu, Fatih M. Uckun, and Rama K. Narla

Subjects
Stereochemistry, Lymphoblastic Leukemia, Clinical Biochemistry, Tetrazolium Salts, Pharmaceutical Science, Antineoplastic Agents, Medicinal chemistry, Biochemistry, Chemical synthesis, Arsenicals, chemistry.chemical_compound, Drug Discovery, Tumor Cells, Cultured, Humans, Cell Lineage, Molecular Biology, Leukemia, Azo compound, Bicyclic molecule, Organic Chemistry, Arsonic acid, General Medicine, Phenylarsonic acid, Precursor Cell Lymphoblastic Leukemia-Lymphoma, Genes, p53, In vitro, Thiazoles, chemistry, Cell culture, Molecular Medicine
Abstract

A series of 12 organic arsonic acid compounds has been synthesized and evaluated against human B-lineage (NALM-6) and T-lineage (MOLT-3) acute lymphoblastic leukemia (ALL) cell lines. The lead compounds 2-trichloromethyl-4-[4'-(4"-phenylazo)phenylarsonic acid]aminoquinazoline (compound 19, PHI-P518; IC(50)=1.1+/-0.5 microM against NALM-6 and 2.0+/-0.8 microM against MOLT-3) and 2-methylthio-4-(2'-phenylarsonic acid)aminopyrimidine (compound 15, PHI-P381; IC(50)=1.5+/-0.3 microM against NALM-6 and 2.3+/-0.5 microM against MOLT-3) exhibited potent antileukemic activity at low micromolar concentrations.

Published
2003
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3. Cysteine chloromethyl and diazomethyl ketone derivatives with potent anti-leukemic activity

Author

David A. Perrey, Rama K. Narla, and Fatih M. Uckun

Subjects
Ketone, Stereochemistry, medicine.drug_class, Clinical Biochemistry, Tetrazolium Salts, Pharmaceutical Science, Antineoplastic Agents, Carboxamide, Biochemistry, Chemical synthesis, Amino Acid Chloromethyl Ketones, Cell Line, Drug Discovery, Tumor Cells, Cultured, medicine, Humans, Cysteine, Coloring Agents, Cytotoxicity, Molecular Biology, IC50, chemistry.chemical_classification, Organic Chemistry, Precursor Cell Lymphoblastic Leukemia-Lymphoma, Haloketone, Thiazoles, chemistry, embryonic structures, cardiovascular system, Molecular Medicine, Tumor Suppressor Protein p53, Aliphatic compound
Abstract

A series of cysteine diazomethyl- and chloromethyl ketone derivatives has been synthesized and evaluated against human B-lineage (Nalm-6) and T-lineage (Molt-3) acute lymphoblastic leukemia cell lines. The chloromethyl ketone compounds showed potent cytotoxicity against these cell lines, with IC50 values in the low micromolar range. The best compounds were N-acetyl-S-dodecyl-Cys chloromethyl ketone (IC50 = 2.0 microM against Nalm-6, 2.3 microM against Molt-3) and N-acetyl-S-trans,trans-farnesyl-Cys chloromethyl ketone (IC50 = 3.0 microM against Nalm-6 and 1.4 microM against Molt-3).

Published
2000
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