Research Triangle Institute

Other

Johns Hopkins University

New York University

Mansukh C Wani

Monroe E Wall

Govindarajan Manikumar

Allan W Nicholas

C Edgar Cook

Yue-Wei Lee

John A Kepler

Jerry R Reel

Dolatrai M Vyas

Neelakantan Balasubramanian

C Ray Tallent

Douglas Rector

Patricia A Fail

Michael A Wall

Yves Pommier

Robert E Miller

Theresa A Shapiro

David J Adams

Michael P Gamcsik

Y-w Lee

O Michael Colvin

Yun W Lee

Beppino C Giovannella

Leroy F Liu

Milan Potmesil

Monroe C Wall

Robert F Silber

Annette L Bodley

Robert R Engle

John R Stephens

Pingsheng Zhang

Camptothecin analogs having an E-ring ketone are effective anti tumor compounds. These compounds inhibit the enzyme topoisomerase I and may alkylate DNA of the associated topoisomerase I DNA cleavable complex.

Camptothecin analogs having an E-ring ketone

Methods of forming camptothecin compounds which are effective anti-tumor compounds are disclosed. These compounds inhibit the enzyme topoisomerase I and may alkylate DNA of the associated topoisomerase I-DNA cleavable complex.

7-substituted camptothecin and camptothecin analogs and methods for producing the same

An androgenic steroid compound of the formula:wherein:

Androgenic steroid compounds and a method of making and using the same

Camptothecin compounds which are effective anti-tumor compounds are disclosed. These conjugates inhibit the enzyme topoisomerase I and enhance the stability of the topoisomerase I-DNA cleavable complex.

Camptothecin compounds with a thioether group

&bgr;-Alanine esters of camptothecin compounds which are effective anti-tumor compounds are disclosed. These compounds inhibit the enzyme topoisomerase I and may alkylate DNA of the associated topoisomerase I-DNA cleavable complex.

Camptothecin &bgr;-alanine esters with topoisomerase I inhibition

Camptothecin compounds having a C,O&mdash;(CF,),O group where n is 1 or 2 are effective anti-tumor compounds. These compounds inhibit the enzyme topoisomerase I and may alkylate DNA of the associated topoisomerase I-DNA cleavable complex.

10, 11-difluoromethylenedioxycamptothecin compounds with topoisomerase I inhibition

Non-toxic camptothecin prodrugs are prepared by esterifying the 20-position hydroxyl group of camptothecin derivatives.

Water-soluble esters of camptothecin compounds

Camptothecin compounds having a --CH.sub.2 --L group are effective anti-tumor compounds. These compounds inhibit the enzyme topoisomerase I and DNA of associated topoisomerase I-DNA complexes.

Camptothecin compounds with combined topoisomarase I inhibition and DNA

An androgenic steroid compound of the formula: ##STR1## wherein: X, Y, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are as defined herein.

Hexahydroindenopyridine compounds having the following formula and relative stereochemistry ##STR1## where R.sup.1 is C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is carboxyl or a group which is metabolized to a carboxyl group under mammalian physiological conditions; R.sup.4 is halogen; mixtures of said compound and acid addition salts thereof exhibit potent antispermatogenic activity and are useful in a method of inhibiting spermatogenesis in mammals.

Hexahydroindenopyridine compounds having antispermatogenic activity

Camptothecin compounds with combined topoisomerase I inhibition and DNA

Growing community of inventors

Durham, NC, United States of America

Mansukh C Wani