Bionumerik Pharmaceuticals, Inc.

Evestra, Inc.

Kesavaram Narkunan

Harry Kochat

Xinghai Chen

Frederick H Hausheer

Klaus Nickisch

James W Cessac

Pemmaraju Narasimha Rao

Qiuli Huang

Bindu Santhamma

Pavankumar Nv Petluru

Ye Wu

Jianyan Wang

Baishakhi Das

Pavankumar N V Petluru

Baishakhi Debnath

James Cessac

Described herein are compounds which exhibit progesterone antagonistic effects and methods of treating cancer using such compounds.

Progesterone antagonists

Described herein are 3-(6,6-ethylene-17&#x3b2;-hydroxy-3-oxo-17&#x3b1;-pregna-4-ene-17&#x3b1;-yl)propionic acid &#x3b3;-lactone derivatives having progestational and aldosterone antagonistic activity. Also described herein are methods of preparing and using these novel compounds.

Progestational 3-(6,6-ethylene-17B-hydroxy-3-oxo-17A-pregna-4-ene-17A-yl)propionic acid G-lactones

Disclosed herein are novel platinum-based analogs possessing two nitrile substituent groups (bis-nitrile) covalently-bonded to the platinum. Also disclosed herein are the reaction schemes for the synthesis of said platinum complexes, as well as quantitative in vitro IC50 data.

Platinum analogs with bis-nitrile-containing ligands

The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW&#x3c;600).

C10-substituted camptothecin analogs

The novel C7-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW&#x3c;600).

C7-substituted camptothecin analogs

A process for synthesizing highly lipophilic derivatives of camptothecin. The process includes reacting dissolved, underivatized camptothecin with a silylated heterocyclic compound in a modified Minisci-type alkylation reaction to produce 7-substituted derivatives of camptothecin.

Process for making camptothecin derivatives

A process for synthesizing highly lipophilic derivatives of camptothecin. The process includes reacting dissolved, underivatized camptothecin with an aldehyde in a modified Minisci-type alkylation reaction to produce 7-substituted derivatives of camptothecin.

Growing community of inventors

San Antonio, TX, United States of America

Kesavaram Narkunan