Catholic Healthcare West

California Pacific Medical Center

Sutter West Bay Hospitals

Other

Sutter West Bay Hospital

Dignity Health

Catholic Healthcare West, Dba St. Mary's Medical Center

Catholic Healthcare West, Doing Business as St. Mary's Medical Center

Li-Xi Yang

Xiandao Pan

Huijuan Wang

Huijan Wang

Xiando Pan

Hui-Juan Wang

Provided herein are compounds, compositions, and methods for treating cancer in a subject in need thereof.

Podophyllotoxin derivatives and their use

Camptothecin-based compounds are useful for treating a neoplasm in mammalian subjects by administering such compound to the subjects in combination with radiotherapy, i.e., the treatment of tumors with radioactive substances or radiation from a source external to the subject. Camptothecin-based compounds are modified by positioning at least one electron-affinic group around the camptothecin structure to enhance their value in combination with radiotherapy. New Camptothecin-based compounds are disclosed that are useful for treating cancer by administering the novel compounds alone or in combination with radiotherapy.

Camptothecin derivatives as chemoradiosensitizing agents

4-O esters of podophyllotoxin and 4'-demethylepipodophyllotoxin are provided. The compounds are 4-O esters of an alkanoic acid or substituted alkanoic acid and podophyllotoxin and 4&#x2032;-demethylepipodophyllotoxin. The compounds are useful for treating cancer.

Podophyllotoxin derivatives

(20S) esters of camptothecin analogs are provided. The compounds are (20S) esters of an oxyalkanoic acid and camptothecin, whichisareoptionally substituted at the 7, 9, 10, 11, and 12 positions of the camptothecin ring. The compounds are useful for treating cancer.

Camptothecin derivatives

(20) esters of camptothecin analogs are provided. The compounds are (20) esters of an aminoalkanoic acid or an imidoalkanoic acid and homocamptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the homocamptothecin ring. The compounds are useful for treating cancer.

Nitrogen-based homo-camptothecin derivatives

(20S) esters of camptothecin analogs are provided. The compounds are (20S) esters of an aminoalkanoic acid or an imidoalkanoic acid and camptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the camptothecin ring. The compounds are useful for treating cancer.

Nitrogen-based camptothecin derivatives

Certain N-deacetylcolchicine and N-deacetylthiocolchine derivatives are described wherein the 7-N position on the B ring is substituted with the group &mdash;C(O)&mdash;(CHR ) &mdash;AR, wherein m is an integer of 0-10, A is S, O, N or a covalent bond; R is substituted phenyl or substituted benzoyl; optionally substituted cycloalkyl of 3-7 carbons; optionally substituted naphtyl; an optionally substituted imide ring; an optionally substituted 5 or 6 member heterocycle with at least one N, S, or O in the ring; or an optionally substituted fused heterocyclic or fused carboxyclic ring system; R (at the 2-position of the A ring) is methoxy, hydroxy, or methylenedioxy when taken together with R ; R (at the 3-position of the A ring) is methoxy, hydroxy, a monosaccharide radical, or is methylenedioxy when taken together with R ; and R is H or is H or methyl when m is 1. Also dimers of such compounds are disclosed. When combined with suitable pharmaceutical excipients, these compounds are useful for treating various types of cancer.

Colchicine derivatives

Novel nitroimidazole compounds are provided that have a substituent linked via an ester linkage. The ester linkage may be obtained by derivation of the hydroxyl group of metronidazole. These nitroimidazole ester analogs have anti-microbial activity, with a number of novel compounds having an anti-microbial activity that is significantly improved with respect to metronidazole. Two particularly preferred embodiments are shown by Formulas 4 and 5 below:

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San Francisco, CA, United States of America

Li-Xi Yang