29111-46-4Relevant articles and documents
CATHEPSIN-D AND ANGIOGENESIS INHIBITORS AND COMPOSITIONS THEREOF FOR TREATING BREAST CANCER
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Page/Page column 18, (2018/09/28)
The invention relates to Cathepsin-D and angiogenesis inhibitors and compositions thereof for treating breast cancer. More particularly, the invention relates to the design and synthesis of inhibitors of Cathepsin D which exhibits antiproliferative activity and also inhibits angiogenesis. The present invention also relates to the compositions thereof for treating breast cancer.
Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure
Okawa, Tomohiro,Aramaki, Yoshio,Yamamoto, Mitsuo,Kobayashi, Toshitake,Fukumoto, Shoji,Toyoda, Yukio,Henta, Tsutomu,Hata, Akito,Ikeda, Shota,Kaneko, Manami,Hoffman, Isaac D.,Sang, Bi-Ching,Zou, Hua,Kawamoto, Tetsuji
, p. 6942 - 6990 (2017/09/07)
A novel class of therapeutic drug candidates for heart failure, highly potent and selective GRK2 inhibitors, exhibit potentiation of β-adrenergic signaling in vitro studies. Hydrazone derivative 5 and 1,2,4-triazole derivative 24a were identified as hit compounds by HTS. New scaffold generation and SAR studies of all parts resulted in a 4-methyl-1,2,4-triazole derivative with an N-benzylcarboxamide moiety with highly potent activity toward GRK2 and selectivity over other kinases. In terms of subtype selectivity, these compounds showed enough selectivity against GRK1, 5, 6, and 7 with almost equipotent inhibition to GRK3. Our medicinal chemistry efforts led to the discovery of 115h (GRK2 IC50 = 18 nM), which was obtained the cocrystal structure with human GRK2 and an inhibitor of GRK2 that potentiates β-adrenergic receptor (βAR)-mediated cAMP accumulation and prevents internalization of βARs in β2AR-expressing HEK293 cells treated with isoproterenol. Therefore, 115h appears to be a novel class of therapeutic for heart failure treatment.
Transition metal complexes of novel ethyl pyruvate hydrazones as potential antitumor agents: Synthesis and physicochemical properties, DNA interactions and antiproliferative activity
Pathan, Aishakhanam H.,Gudasi, Kalagouda B.
, p. 1504 - 1516 (2013/05/08)
A new series of ethyl pyruvate hydrazones and their later first row transition metal(II) complexes have been synthesized and characterized by means of elemental analyses, vibrational, electronic, 1H and 13C NMR, electron paramagnetic resonance, and mass spectroscopic techniques along with thermal and magnetic studies. All complexes were found to be monomeric in nature and have octahedral geometry. The prepared compounds were evaluated for antiproliferative activity against the two human cancer cell lines (HeLa and HepG2). The Cu(II) complexes were found to have potential activity against the cell lines used than the ligand and other complexes. In addition, the DNA-binding/cleaving capacity of the compounds were analyzed by absorption spectroscopy, viscosity measurement, thermal denaturation studies and gel electrophoresis methods.