University of Puerto Rico

Linette Castillo-Pichardo

Cornelis P Vlaar

Suranganie Dharmawardhane Flanagan

Eliud Hernandez-O'Farrill

Eliud Hernandez-o'farrill

Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

1,5-disubstituted 1,2,3-triazoles are inhibitors of Rac/CDC42 GTPases

A series of novel EHop-016 derivatives is presented herein via designing and synthesizing compounds that mimics its more favorable 'U-shaped' conformation that appears to be critical for inhibitory activity against Rac. Based on modeling studies on EHop-016, compounds with a more rigid structural conformation can mimic this 'U-shaped' conformation and would improve the anti-migration activity against metastatic cells. Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases, for instance compounds of formula  Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

Carbazole EHop-016 derivatives as anticancer and anti-migratory agents

Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperproliferative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

1,5-disubstituted 1,2,3-triazoles are inhibitors of Rac/Cdc42 GTPases

1,5-disubstituted 1,2,3-triazoles are inhibitors of RAC/CDC42 GTPases

A series of novel EHop-016 derivatives is presented herein via designing and synthesizing compounds that mimics its more favorable 'U-shaped' conformation that appears to be critical for inhibitory activity against Rac. Based on modeling studies on EHop-016, compounds with a more rigid structural conformation can mimic this 'U-shaped' conformation would improve the anti-migration activity against metastatic cells. Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases, for instance compounds of formula (I)  Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

Growing community of inventors

San Juan, Puerto Rico

Linette Castillo-Pichardo