Inhibitors of phosphatidylinositol-3-kinase (PI3) and inducers of nitric oxide (NO)

摘要

The present invention relates to compounds of general formula 1 for the treatment of malignancy by inhibition of PI3-Akt pathway and or induction of NO. The present invention also relates to the use of compound of general formula 1 for the treatment of malignancy by inhibition of PI3-Akt pathway and or induction of NO. The present invention further relates to a method of treating malignancy by inhibition of PI3-Akt pathway and or induction of NO by administration of compound or said composition to a mammal in need thereof.

主权项

1. A compound of general formula 1: wherein R1 is one of H or COCH3, and R2 is H or COCH3, or R1 and R2 combine to form —CH2—; R3 is one of H or CH2—CH═CH2, and R4 is one of H, CH2—CH═CH2, CH2—CH2—CH3, C(CH3)2CH═NOH, C(CH3)2CH═CH2, C(CH3)2CN, or C(CH3)2CH═NOCOCH3,
whereinin the case that R3 is H, then R4 is CH2—CH2—CH3,C(CH3)2CH═NOH, C(CH3)2CH═CH2, C(CH3)2CN orC(CH2)2CH═NOCOCH3, andin the case that R3═CH2—CH═CH2, then R4 is CH2—CH═CH2, CH2—CH2—CH3, C(CH3)2CH═NOH, C(CH3)2CH═CH2, C(CH3)2CN orC(CH3)2CH═NOCOCH3; R5 is one of H or CH2—CH═CH2; R6 is one of H or CH2—CH═CH2;
whereinin the case that R4 is CH2—CH3—CH3, then R3 or R5 is CH3—CH═CH2;in the case that R4 and R3 combine to form —CH3—, then R4 is C(CH3)2CH═CH2; andin the case that R1 and R2 are each H, then R4 is one of C(CH2)2CH═NOH, C(CH3)3CN or CH3—CH3—CH3.