摘要:
Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.
摘要:
Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.
摘要:
Oligoamine compounds with anti-cancer and anti-proliferative activity are provided, as well as methods for making and using the compounds. The compounds are shown to be active against prostate cancer cell lines and against prostate cancer tumors in mice. The compounds are also useful in treatment of breast cancer and other cancers.
摘要:
Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.
摘要:
Porphyrin-polyamine conjugate compounds are disclosed which have anticancer and antitumor effects. The porphyrin moiety selectively localizes in tumors, while the polyamine moiety serves as a cytotoxic agent. Methods of making and using the porphyrin-polyamine conjugate compounds are also disclosed.
摘要:
Novel quinones are provided, as well as compositions comprising these novel quinones. Methods of using the novel quinones in treatment of various indications including cancer are also provided.
摘要:
Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to, porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.
摘要:
Novel cyclic polyamine compounds of the form where A1, each A2 (if present), and A3 are independently selected from C1-C8 alkyl, where each Y is independently selected from H or C1-C4 alkyl, where M is selected from C1-C4 alkyl, where k is 0, 2, or 3, and where R is selected from C1-C32 alkyl, as well as all stereoisomers and salts thereof, are disclosed. Additional compounds where k is 1 and A2 is independently selected from C1-C3 alkyl or C5-C8 alkyl are also disclosed. Cyclic polyamines, where the amide group is reduced to a secondary amino group, and various derivatives of these compounds, are also described. Synthetic methods for the compounds are described. The compounds are useful for treating diseases caused by uncontrolled proliferation of cells, such as cancer, especially prostate cancer, and for inducing intracellular ATP hydrolysis for treatment of other disorders.
摘要翻译:其中A 1 A 1,每个A 2(如果存在)和A 3 N 3的形式的新型环状多胺化合物独立地选自C SUB 其中每个Y独立地选自H或C 1 -C 4烷基,其中M(C 1 -C 4)烷基,其中每个Y独立地选自H或C 1 -C 4烷基,其中M 选自C 1 -C 4烷基,其中k是0,1,2或3,并且其中R选自C 1 -C 4 - C 32烷基,以及其全部立体异构体和盐。 其中k为1且A 2 H 2的其它化合物独立地选自C 1 -C 3烷基或C 5 - -C 8烷基也被公开。 还描述了其中酰胺基还原为仲氨基的环状多胺,以及这些化合物的各种衍生物。 描述了化合物的合成方法。 该化合物可用于治疗由不受控制的细胞增殖(例如癌症,特别是前列腺癌)引起的疾病,并用于诱导细胞内ATP水解以治疗其他疾病。
摘要:
Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions comprising these conjugates. Methods of using these conjugates in the treatment of prostate diseases are also provided.
摘要:
Porphyrin-polyamine conjugate compounds are disclosed which have anticancer and antitumor effects. The porphyrin moiety selectively localizes in tumors, while the polyamine moiety serves as a cytotoxic agent. Methods of making and using the porphyrin-polyamine conjugate compounds are also disclosed.