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US 2018/0002355 A1Published application
Benzocyclooctene-based and indene-based anticancer agents
AssigneeBaylor University
InventorsKevin G. PINNEY, Christine A. HERDMAN, Rajendra P. TANPURE, Zhi CHEN
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Abstract
Benzocyclooctene (fused 6,8 ring system) analogues and corresponding indene (fused 6,5 ring system) analogues function as inhibitors of tubulin polymerization. The compounds are useful as anticancer agents in a new therapeutic approach for cancer treatment utilizing small-molecule inhibitors of tubulin polymerization that also act as vascular disrupting agents (VDAs).
Claims17
A benzocyclooctene compound demonstrating inhibition of tubulin polymerization and having a structure of:
- wherein
- A is a bond, C═O, C═NH, or C═NR1, where R1 is any alkyl, aryl, or alkaryl substituent;
- B is CH2, NH, O, S, CH—OH, or CH—OR2, wherein R2 is CH3, or PO3−, or C-Z, wherein Z is halogen;
- and
- D is CH, N, C—OH, or C—OR3, wherein R3 is CH3, any alkyl substituent, any alkoxy substituent, any alkyl or alkoxy substituent including heteroatoms, any carbonyl substituent, any ester substituent, or PO3−, or C-Z, wherein Z is halogen.
2 more elements
An indene compound demonstrating inhibition of tubulin polymerization and having a structure of:
- wherein
- A is a bond, C═O, C═NH, or C═NR1, where R1 is any alkyl, aryl, or alkaryl substituent;
- B is CH2, NH, O, S, CH—OH, or CH—OR2, wherein R2 is CH3, or PO3−, or C-Z, wherein Z is halogen;
- and
- D is CH, N, C—OH, or C—OR3, wherein R3 is CH3, any alkyl substituent, any alkoxy substituent, any alkyl or alkoxy substituent including heteroatoms, any carbonyl substituent, any ester substituent, or PO3−, or C-Z, wherein Z is halogen, and wherein at least one D is C—OH or C—OPO32−.
2 more elements
Dependencies are inferred from the claim text.