Synthesis of nitrogen-containing derivatives of 17(20)-pregnenoic, 17β-hydroxypregnanoic, and 17α-hydroxypregnanoic acids as new potential antiandrogens

Derivatives of 3β-hydroxyandrost-5,16-diene and 3β-hydroxyandrost-5-ene containing 2-oxazoline, 2-benzoxazole, and 2-benzimidazole substituents at C-17 position were synthesized. Docking of the synthesized compounds into the active site of human CYP17A1 predicted their high affinity for the enzyme. Of the 6 new compounds, 5 suppressed the proliferation of prostate carcinoma cells LNCaP and PC-3, and the activity of the oxazoline and benzimidazole derivatives of androsta-5,16-diene significantly exceeded the activity of the known anticancer agents abiraterone and galeterone.

show abstract

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

customersupport@researchsolutions.com

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

Synthesis of nitrogen-containing derivatives of 17(20)-pregnenoic, 17β-hydroxypregnanoic, and 17α-hydroxypregnanoic acids as new potential antiandrogens

Cited by 3 publications

References 35 publications

Oxazoline derivatives of [17(20)E]-21-norpregnene – inhibitors of CYP17A1 activity and proliferation of prostate carcinoma cells

Oxazoline derivatives of [17(20)E]-21-norpregnene – inhibitors of CYP17A1 activity and proliferation of prostate carcinoma cells

Synthesis, anti-leukemia activity, and molecular docking of novel 3,16-androstenedione derivatives

New Nitrogen-containing Androstane Derivatives Suppressing Prostate Carcinoma Cells Proliferation

Contact Info

Product

Resources

About