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Enzymatic stability, solution structure, and antiproliferative effect on prostate cancer cells of leuprolide and new gonadotropin-releasing hormone peptide analogs.
Analogs of GnRH, including [DLeu6, desGly1o]-GnRH-NHEt (leuprolide, commercial product), have been widely used in oncology to induce reversible chemical castration. Several studies have provided… Expand
Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies.
- Panagiotis Zoumpoulakis, C. Camoutsis, +4 authors A. Pitsas
- Chemistry, Medicine
- Bioorganic & medicinal chemistry
- 15 February 2012
The significant antifungal activity of a series of sulfonamide-1,2,4-triazole and 1,3,4-thiazole derivatives against a series of micromycetes, compared to the commercial fungicide bifonazole has been… Expand
Structural studies and cytotoxicity assays of “aggregation‐prone” IAPP8–16 and its non‐amyloidogenic variants suggest its important role in fibrillogenesis and cytotoxicity of human amylin
- Nikolaos N. Louros, Paraskevi L Tsiolaki, +8 authors S. Hamodrakas
- Chemistry, Medicine
- 1 May 2015
Amyloid deposits to the islets of Langerhans are responsible for the gradual loss of pancreatic β‐cells leading to type II diabetes mellitus. Human mature islet amyloid polypeptide (hIAPP), a… Expand
Further studies on the antineoplastic activity of homo-aza-steroidal esters.
The modified steroidal alkylating agents, 17 beta-hydroxy-3-aza-A-homo-4 alpha-androsten-4- one(p-[bis(2-chloroethyl)amino]phenyl)butyrate(1),3 alpha-hydroxy- 13,17-seco-5 alpha- butyrate(2),3… Expand
A new route for the synthesis of steroidal esters of carboxylic derivatives of N,N-bis(2-chloroethyl) aniline with DCC
Synthesis of a new nor-aza-steroidal ester of p-N,N-bis-(2-chloroethyl)aminophenylbutyric acid and in vitro study of its mutagenicity and clastogenicity.
A new nor-aza-steroidal ester of chlorambucil has been synthesized. The study of the mitotic index in CHO and HeLa cells treated with this compound showed that it may be a cytostatic drug. It was… Expand
On the formation of estrone lactam esters of N,N‐bis(2‐chloroethyl)aminocinnamic acid isomers, p‐N,N‐bis(2‐chloroethyl)aminophenylbutyric acid and their antitumor activity
New estrone-lactam esters, 17α-aza-D-homo-Δ1,3,5(10)-estratrien-3-ol-17-one-N,N-bis(2-chloroethyl)-aminocinnamic isomers and p-N,N-bis(2-chloroethyl)aminophenylbutyrate have been synthesized and… Expand
Assessment of anti-HIV and antiproliferative activity of homo-aza-steroidal esters in culture