20949-81-9Relevant articles and documents
Heterocycles 38. Biocatalytic synthesis of new heterocyclic mannich bases and derivatives
Leonte, Denisa,Bencze, László Csaba,Paizs, Csaba,Irimie, Florin Dan,Zaharia, Valentin
, p. 12300 - 12313 (2015)
This paper describes the biocatalytic synthesis of new Mannich bases containing various heterocyclic rings (thiazole, furane, thiophene, pyridine) by applying the lipase catalyzed trimolecular condensation of the corresponding heterocyclic aldehydes with acetone and primary aromatic amines, in mild and eco-friendly reaction conditions. The obtained Mannich bases were acylated to their corresponding N-acetyl derivatives. All compounds were characterized by 1H-NMR, 13C-NMR and MS spectrometry.
TRANSCRIPTION FACTOR BRN2 INHIBITORY COMPOUNDS AS THERAPEUTICS AND METHODS FOR THEIR USE
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Page/Page column 89; 90, (2020/05/15)
The invention provides a variety of compounds having the structure of Formula I and uses of such compounds for treatment of various indications, including cancer as well as methods of treatment involving such compounds are also provided. The uses of the compounds may specifically include: bladder cancer, cholangiocarcinoma; colorectal cancer; diffuse large B-cell lymphoma (DLBC); liver cancer; ovarian cancer; thymoma; thyroid cancer; clear cell renal cell carcinoma (CCRCC); chromophobe renal cell carcinoma (ChRCC); prostate cancer; breast cancer; uterine cancer; pancreatic cancer; cervical cancer; uveal melanoma; acute myeloid leukemia (AML); head and neck cancer; small cell lung cancer (SCLC); lung adenocarcinoma sarcoma; mesothelioma; adenoid cystic carcinoma (ACC), sarcoma; testicular germ cell cancer; uterine cancer; pheochromocytoma and paraganglioma (PCPG); melanoma; glioma; glioblastoma multiforme; T-cell Acute Lymphoblastic Leukemia; T-cell Lympohoma, medulloblastoma; and neuroblastoma.
Heterocycles 44. Synthesis, characterization and anticancer activity of new thiazole ortho-hydroxychalcones
Coman, Fana-Maria,Mbaveng, Armelle T.,Leonte, Denisa,Bencze, László Csaba,Vlase, Laurian,Imre, Silvia,Kuete, Victor,Efferth, Thomas,Zaharia, Valentin
, p. 1396 - 1407 (2018/03/06)
A novel series of substituted thiazole ortho-hydroxychalcones was synthesized to be physico-chemically characterized and evaluated for the anticancer activity. The chalcones were synthesized with 28–68% yields, via Claisen–Schmidt condensation in an ethanolic solution. All the synthesized compounds were purified and characterized by MS, 1H NMR, 13C NMR, IR, and melting points. The cytotoxicity of thiazole ortho-hydroxychalcones 3a–3o as well as doxorubicin was determined in a panel of 9 cancer cell lines including sensitive and drug resistant phenotypes. Compounds 3a, 3b, 3c, 3j, as well as doxorubicin displayed cytotoxic effects in all the 9 tested cancer cell lines with IC50 values below 75 μM. The best samples showed IC50 values below 10 μM against 5/9 cancer cell lines for 3a, 3h, and 3o, against 7/9 cancer cell lines for 3c and 3f, and against 8/9 cancer cell lines for 3j. Hypersensitivity of all resistant cells towards 3b, 3g, 3j, 3m, and 3o was also obtained, suggesting that these compounds are appropriate molecules that could be used to combat drug resistance of cancer cells.