公开(公告)号：US08609858B2

公开(公告)日：2013-12-17

申请号：US12921061

申请日：2009-03-05

申请人： Mahabalarao Sampath Kumar Halmuthur ,  Ajit Kumar Saxena ,  Subhash Chandra Taneja ,  Shashank Kumar Singh ,  Vijay Kumar Sethi ,  Naveed Ahmed Qazi ,  Sanghapal Damodhar Sawant ,  Mahendhar Reddy Doma ,  Abid Hussain Banday ,  Monika Verma ,  Ghularn Nabi Qazi

发明人： Mahabalarao Sampath Kumar Halmuthur ,  Ajit Kumar Saxena ,  Subhash Chandra Taneja ,  Shashank Kumar Singh ,  Vijay Kumar Sethi ,  Naveed Ahmed Qazi ,  Sanghapal Damodhar Sawant ,  Mahendhar Reddy Doma ,  Abid Hussain Banday ,  Monika Verma ,  Ghularn Nabi Qazi

IPC分类号： C07D498/10 ,  C07D491/107

CPC分类号： C07D491/107 ,  C07D498/10

摘要： The present invention relates to novel spiro derivatives of parthenin prepared by the dipolar cycloaddition of various dipoles viz, benzonitrile oxides, nitrones, azides, nitrile ylide diazoalkane, nitrile imide, ozone, azomethine imides, azomethine ylides etc. with exocyclic double bond of C ring (α-methylene-γ-butyrolactone). Representative compounds have been screened for their anticancer activity against different cancer cell lines. ICs0 value of these analogues varies between 4.3 μM to 93 μM. A mechanistic correlation of their anticancer activity has been described. The results of the cytotoxicity test of the compounds studies indicated that the α,β-unsaturated ketonic moiety in parthenin plays an important role in the maintenance of the high level of cytotoxicity.

摘要翻译： 本发明涉及通过各种偶极子，苄腈氧化物，硝酮，叠氮化物，腈基内鎓，重氮烷，腈酰亚胺，臭氧，偶氮甲碱酰亚胺，偶氮甲碱基内鎓等与环C的环外双键的偶极环加成制备的新戊二烯衍生物 （α-亚甲基-γ-丁内酯）。 已经筛选了代表性化合物对抗不同癌细胞系的抗癌活性。 这些类似物的ICs0值在4.3μM至93μM之间变化。 已经描述了其抗癌活性的机械相关性。 化合物研究的细胞毒性试验的结果表明，单分散素中的α，β-不饱和酮部分在维持高水平的细胞毒性中起重要作用。

公开(公告)号：US20110201661A1

公开(公告)日：2011-08-18

申请号：US12921061

申请日：2009-03-05

申请人： Mahabalarao Sampath Kumar Halmuthur ,  Ajit Kumar Saxena ,  Subhash Chandra Taneja ,  Shashank Kumar Singh ,  Vijay Kumar Sethi ,  Naveed Ahmed Qazi ,  Sanghapal Damodhar Sawant ,  Mahendhar Reddy Doma ,  Abid Hussain Banday ,  Monika Verma ,  Ghularn Nabi Qazi

发明人： Mahabalarao Sampath Kumar Halmuthur ,  Ajit Kumar Saxena ,  Subhash Chandra Taneja ,  Shashank Kumar Singh ,  Vijay Kumar Sethi ,  Naveed Ahmed Qazi ,  Sanghapal Damodhar Sawant ,  Mahendhar Reddy Doma ,  Abid Hussain Banday ,  Monika Verma ,  Ghularn Nabi Qazi

IPC分类号： A61K31/424 ,  C07D498/10 ,  C07D491/107 ,  A61K31/396 ,  A61P35/00

CPC分类号： C07D491/107 ,  C07D498/10

摘要： The present invention relates to novel spiro derivatives of parthenin prepared by the dipolar cycloaddition of various dipoles viz, benzonitrile oxides, nitrones, azides, nitrile ylide diazoalkane, nitrile imide, ozone, azomethine imides, azomethine ylides etc. with exocyclic double bond of C ring (α-methylene-γ-butyrolactone). Representative compounds have been screened for their anticancer activity against different cancer cell lines. ICs0 value of these analogues varies between 4.3 μM to 93 μM. A mechanistic correlation of their anticancer activity has been described. The results of the cytotoxicity test of the compounds studies indicated that the α,β-unsaturated ketonic moiety in parthenin plays an important role in the maintenance of the high level of cytotoxicity.

摘要翻译： 本发明涉及通过各种偶极子，苄腈氧化物，硝酮，叠氮化物，腈基内鎓，重氮烷，腈酰亚胺，臭氧，偶氮甲碱酰亚胺，偶氮甲碱基内鎓等与环C的环外双键的偶极环加成制备的新戊二烯衍生物 （α-亚甲基-γ-丁内酯）。 已经筛选了代表性化合物对抗不同癌细胞系的抗癌活性。 这些类似物的ICs0值在4.3μM至93μM之间变化。 已经描述了其抗癌活性的机械相关性。 化合物研究的细胞毒性试验结果表明，在维持高水平的细胞毒性方面，单分散素中α，bgr-不饱和酮部分起重要作用。