287407-07-2Relevant academic research and scientific papers
Design, synthesis, and in?vitro evaluation of BP-1-102 analogs with modified hydrophobic fragments for STAT3 inhibition
Oleksak, Patrik,Psotka, Miroslav,Vancurova, Marketa,Sapega, Olena,Bieblova, Jana,Reinis, Milan,Rysanek, David,Mikyskova, Romana,Chalupova, Katarina,Malinak, David,Svobodova, Jana,Andrys, Rudolf,Rehulkova, Helena,Skopek, Vojtech,Ngoc Lam, Pham,Bartek, Jiri,Hodny, Zdenek,Musilek, Kamil
, p. 410 - 424 (2021/02/05)
Twelve novel analogs of STAT3 inhibitor BP-1-102 were designed and synthesised with the aim to modify hydrophobic fragments of the molecules that are important for interaction with the STAT3 SH2 domain. The cytotoxic activity of the reference and novel co
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia
Bukhari, Shazreh,Cabral, Aaron D.,De Araujo, Elvin D.,Gawel, Justyna M.,Gunning, Patrick T.,He, Liying,Johns, Alexandra E.,Manaswiyoungkul, Pimyupa,Nawar, Nabanita,Olaoye, Olasunkanmi O.,Raouf, Yasir S.,Sedighi, Abootaleb,Shouksmith, Andrew E.,Sina, Diana
supporting information, p. 56 - 64 (2020/01/31)
The HDAC inhibitor 4-tert-butyl-N-(4-(hydroxycarbamoyl)phenyl)benzamide (AES-350, 51) was identified as a promising preclinical candidate for the treatment of acute myeloid leukemia (AML), an aggressive malignancy with a meagre 24% 5-year survival rate. Through screening of low-molecular-weight analogues derived from the previously discovered novel HDAC inhibitor, AES-135, compound 51 demonstrated greater HDAC isoform selectivity, higher cytotoxicity in MV4-11 cells, an improved therapeutic window, and more efficient absorption through cellular and lipid membranes. Compound 51 also demonstrated improved oral bioavailability compared to SAHA in mouse models. A broad spectrum of experiments, including FACS, ELISA, and Western blotting, were performed to support our hypothesis that 51 dose-dependently triggers apoptosis in AML cells through HDAC inhibition.
Androgen receptor antagonist as well as preparation method and application thereof
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Paragraph 0058-0060; 0065-0067, (2019/04/02)
The invention relates to an androgen receptor antagonist as well as a preparation method and an application thereof. The androgen receptor antagonist is a compound shown as the general formula (I) inthe description or a pharmaceutically acceptable salt of the compound (R1, R2, R3 and R4 in the general formula are defined in the description).
ACETYLENIC ALPHA-AMINO ACID-BASED SULFONAMIDE HYDROXAMIC ACID TACE INHIBITORS
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Page 65, (2010/02/07)
Compound of the formula (B) are useful in treating disease conditions mediated by TNF- alpha , such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
Acetylenic TACE inhibitors. Part 1. SAR of the acyclic sulfonamide hydroxamates
Levin,Chen,Cheung,Cole,Crago,Delos Santos,Du,Khafizova,MacEwan,Niu,Salaski,Zask,Cummons,Sung,Xu,Zhang,Xu,Ayral-Kaloustian,Jin,Cowling,Barone,Mohler,Black,Skotnicki
, p. 2799 - 2803 (2007/10/03)
The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors, all bearing a butynyloxy P1′ group, was explored. In particular, compound 5j has excellent in vitro potency against isolated TACE enzyme and in cells, good selectivity over MMP-1 and MMP-9, and oral activity in an in vivo model of TNF-α production and a collagen-induced arthritis model.
