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。

公开(公告)号：US20090298938A1

公开(公告)日：2009-12-03

申请号：US12401337

申请日：2009-03-10

申请人： Ghulam Nabi Qazi ,  Subhash Chandra Taneja ,  Jaswant Singh ,  Ajit Kumar Saxena ,  Vijay Kumar Sethi ,  Bhahwal Ali Shah ,  Bal Krishan Kapahi ,  Samar Singh Andotra ,  Ajay Kumar ,  Shashi Bhushan ,  Fayaz Malik ,  Dilip Manikrao Mondhe ,  Shanmugavel Muthiah ,  Surjeet Singh ,  Monika Verma ,  Shashank Kumar Singh

发明人： Ghulam Nabi Qazi ,  Subhash Chandra Taneja ,  Jaswant Singh ,  Ajit Kumar Saxena ,  Vijay Kumar Sethi ,  Bhahwal Ali Shah ,  Bal Krishan Kapahi ,  Samar Singh Andotra ,  Ajay Kumar ,  Shashi Bhushan ,  Fayaz Malik ,  Dilip Manikrao Mondhe ,  Shanmugavel Muthiah ,  Surjeet Singh ,  Monika Verma ,  Shashank Kumar Singh

IPC分类号： A61K31/19 ,  C07C62/30

CPC分类号： A61K31/19

摘要： The present invention relates to use of compounds of general formula 1 for anticancerous activity, wherein the said compound being derived semi-synthetically from natural triterpenoic acids known as boswellic acids by the induction of apoptosis thereof cytotoxicity and anti-cancer activity displayed by semi-synthetic analogues of natural triterpenes, known as Boswellic acids. These compounds may be used for the treatment of cancer, alone or in combination with pharmaceutically acceptable or other carriers, displaying cytotoxicity and anti-cancer activity for colon, prostrate, liver, breast, central nervous system (CNS), leukemia and malignancy of other tissues, including ascites and solid tumors. The cancer cell death is mediated by induction of apoptosis and inhibition of cell proliferation at specific doses.

摘要翻译： 本发明涉及通式1的化合物用于抗癌活性的用途，其中所述化合物通过诱导其细胞凋亡的细胞毒性和半合成显示的抗癌活性而被天然三萜烯酸被称为保乳酸半合成衍生 天然三萜类似物，称为乳香酸。 这些化合物可以单独使用或与药学上可接受的或其它载体组合用于治疗癌症，显示对结肠，前列腺癌，肝癌，乳腺癌，中枢神经系统（CNS），白血病和其他恶性肿瘤的细胞毒性和抗癌活性 组织，包括腹水和实体瘤。 癌细胞死亡是通过细胞凋亡的诱导和特定剂量的细胞增殖抑制来介导的。