University of North Carolina at Chapel Hill

Other

National Taiwan University

Kenneth F Bastow

Kuo-Hsiung Lee

Zhiyan Xiao

Hui-Kang Wang

Tian-Shung Wu

Yung-Chi Cheng

Qian Shi

Xin Guo

Xihong Wang

Zheng-Yu Yang

Sheng-Chu Kuo

Che-Ming Teng

Pan-Chyr Yang

Arnold Brossi

Fang-Yu Lee

Yi Xia

Tse-Ming Hong

Shuenn-Chen Yang

Hironari Ohtsu

Xiaoming Yang

Linyi Wei

Yuka Nakanishi

The present invention provides compounds of Formula (I-IV): compositions containing the same, and methods of use thereof such as for the treatment of cancer. 

Antofine and cryptopleurine derivatives as anticancer agents

Compounds of Formula I are described: preferably subject to the proviso that either (a) Rand Rtogether form &#x2014;O&#x2014;CH(R)&#x2014;O&#x2014;, or (b) Rand Rtogether form &#x2014;O&#x2014;CH(R)&#x2014;O&#x2014;, wherein Ris H, halo, or loweralkyl. Pharmaceutical salts, formulations, and methods of using the same in the treatment of cancer are also described. 

Tylophorine analogs as antitumor agents

Compounds of Formulas I-II are described, along with methods of using such compounds for the treatment of cancer and pharmaceutical formulations thereof.

Neo-tanshinlactone and analogs as potent and selective anti-breast cancer agents

Etoposide analogs with improved water-solubility such as 4'-O-Demethyl-4&#x2032;-(N&#x2032;,N&#x2032;-dimethyl-glycyl)-4&#x3b2;-(4&#x2033;-nitroanilino)-4-desoxy-podophyllotoxin (8) and 4&#x2032;-O-Demethyl-4&#x2032;-(N&#x2032;,N&#x2032;-dimethyl-glycyl)-4&#x3b2;-(4&#x2033;-fluoroanilino)-4-desoxy-podophyllotoxin (9) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.

Water-soluble etoposide analogs and methods of use thereof

Compounds of Formulas I-II are described, along with methods of using such compounds for the treatment of cancer and pharmeutical formulations thereof.

Compounds are described having a structure according to Formula I or Formula II:wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O and S; m is from 1 to 3; n is from 1 to 5; Rand Rare each independently selected from the group consisting of H, hydroxy, lower alky, lower alkoxy, halo, amino, aminoalkyl, nitro, heteroaryl, &#x2014;OC(&#x2550;O)R, &#x2014;O(C&#x2550;O)OR; and &#x2014;O(C&#x2550;O)N(R); and Ris side chain such as an acetic acid side chain, where p is O to 4, Ris hydroxy, alkoxy or amino, and Ris H or lower alkyl, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer.

Flavone acetic acid analogs and methods of use thereof

Etoposide analogs such as 4'-O-demethyl-4&#x3b2;-[4&#x2033;-(methyl-L-tyrosine-N-carbonyl)-anilino]-4-desoxy-podophyllotoxin (12) and 4&#x2032;-O-demethyl-4&#x3b2;-[4&#x2033;-(methyl-L-tryptophan-N-carbonyl)-anilino]-4-desoxypodophyllotoxin (13) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.

Etoposide analogs and methods of use thereof

Taxoid conjugates as antimitotic and antitumor agents

Compounds according to formula I: C&prime;&mdash;L&mdash;T (I), wherein C&prime; is a camptothecin group; L is a linking moiety; T is a taxoid group, pharmaceutically acceptable salt thereof. The compounds are useful in, among other things, treating cancer in subjects in need thereof, including cellular differentiation, and inhibiting cellular mitosis.

Camptothecin-taxoid conjugates as antimitotic and antitumor agents

Etoposide analogs such as 4&prime;-O-demethyl-4&bgr;-&lsqb;4&Prime;-(methyl-L-tyrosine-N-carbonyl)-anilino&rsqb;-4-desoxy-podophyllotoxin (12) and 4&prime;-O-demethyl-4&bgr;-&lsqb;4&Prime;-(methyl-L-tryptophan-N-carbonyl)-anilino&rsqb;-4-desoxypodophyllotoxin (13) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.

Covalent conjugates of topoisomerase I and topoisomerase II inhibitors

A novel antiproliferative drug and methods are disclosed. The drug has the general structural formula: ##STR1## where R1=OR.sub.1 ', SR.sub.1 ', or N(R.sub.1 'R.sub.1 ').sub.2, where R.sub.1 ' and R.sub.1 ' are H or lower alkyl groups, and R.sub.2 is an acylamino, or aroylamino group. The compound is useful for inhibiting cell proliferation in drug-resistant tumor cells. Also disclosed is a method of chemical converting a colchicine derivative to form an active inhibitor of DNA topisomerase II.

Growing community of inventors

Chapel Hill, NC, United States of America

Kenneth F Bastow