52480-33-8Relevant academic research and scientific papers
TAM KINASE INHIBITORS
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Paragraph 0175; 0176, (2018/11/10)
Described herein are compounds, methods of making such compounds, compositions (e.g., pharmaceutical compositions/medicaments) that include such compounds, and methods of using such compounds to treat diseases, such as cancer.
Inhibition of cancer cell invasion by new ((3,4-dihydroxy benzylidene)hydrazinyl)pyridine-3-sulfonamide analogs
Kang, Seong-Mook,Nam, Ky-Youb,Jung, Seung-Youn,Song, Kyung-Hee,Kho, Seongho,No, Kyoung Tai,Choi, Hyun Kyung,Song, Jie-Young
, p. 1322 - 1328 (2016/02/23)
Rab GTPases regulate various types of intracellular membrane trafficking in all eukaryotes. Since Rab27a and its multiple effectors are involved in exocytosis of lysosome-related organelles and play a major role in malignancy, compounds targeting Rab27a could be likely used to inhibit invasive growth and tumor metastasis. Thus, we designed and synthesized several compounds based on the previously reported Rab27a-targeting synthetic compounds identified by virtual screening, and investigated their anti-metastatic effects in MDA-MB231 and A375 cells. Among the synthesized compounds, (E)-N-(3-chlorophenyl)-6-(2-(3,4-dihydroxy benzylidene)hydrazinyl)pyridine-3-sulfonamide (3d) and (E)-N-benzyl-6-(2-(3,4-dihydroxy benzylidene)hydrazinyl)-N-methylpyridine-3-sulfonamide (3f) significantly inhibited the invasiveness of both tumor cell lines. Compounds 3d and 3f also decreased the levels of signature extracellular matrix marker proteins (fibronectin, collagen, and α-smooth muscle actin) and representative mesenchymal cell markers (N-cadherin and vimentin). Taken together, our results suggest that novel sulfonamide analogs have anti-metastatic activity in breast and melanoma cancer cell lines and may be used as therapeutic agents to treat malignant cancer.
THERAPUETIC USES OF SELECTED PYRIMIDINE COMPOUNDS WITH ANTI-MER TYROSINE KINASE ACTIVITY
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Page/Page column 195, (2015/11/03)
Uses of pyrimidines with anti-Mer tyrosine kinase activity as anti-infective agents, immunostimulatory and immunomodulatory agents, anti-cancer agents (including against MerTK -/- tumors and ITD and TKD mutant forms of Acute Myeloid Leukemia (AML)), and as adjunctive agents in combination with chemotherapeutic, radiation or other standard of care for neoplasms.
PYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER
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Page/Page column 20; 21, (2014/06/23)
Compounds of Formula I or II: are described, along with pharmaceutical compositions containing the same and methods of using such compounds for the treatment of cancer.
PYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER
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Page/Page column 56; 57, (2014/01/07)
Described are compounds of Formula I or Formula II: wherein: ring A is a 5- or 6-membered heteroaryl group; dashed lines are optional double bonds; X is N or O; Y is a carbon atom or an S or N heteroatom in ring A in any suitable location; and substituents are as given herein. Compositions containing the same and methods of using the same in treating cancers such as acute lymphoblastic leukemia are also described.
Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new mer kinase inhibitors
Zhang, Weihe,Zhang, Dehui,Stashko, Michael A.,DeRyckere, Deborah,Hunter, Debra,Kireev, Dmitri,Miley, Michael J.,Cummings, Christopher,Lee, Minjung,Norris-Drouin, Jacqueline,Stewart, Wendy M.,Sather, Susan,Zhou, Yingqiu,Kirkpatrick, Gregory,Machius, Mischa,Janzen, William P.,Earp, H. Shelton,Graham, Douglas K.,Frye, Stephen V.,Wang, Xiaodong
supporting information, p. 9683 - 9692 (2014/01/06)
Abnormal activation or overexpression of Mer receptor tyrosine kinase has been implicated in survival signaling and chemoresistance in many human cancers. Consequently, Mer is a promising novel cancer therapeutic target. A structure-based drug design appr
NEW COMPOUNDS
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Page/Page column 50, (2008/06/13)
The present invention relates to new compounds of formula Ia or Ib wherein P represents a 5- or 6-membered heteroaromatic ring containing one or two heteroatoms selected independently from N, O and S of which at least one heteroatom is nitrogen; R is hydrogen; R is selected from: C1-6alkyl, cyano, halogen, (CO)OR, and CONRR; R is selected from: C1-6alkyl, cyano, nitro, (CO)OR, C1-6alkylNRR, OC2-6alkylNRR, CONRR, and (SO2)NRR; m is 0, 1, 2, 3 or 4; n is 0, 1, 2, 3 or 4; as a free base or a salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
DIPEPTIDYL PEPTIDASE IV INHIBITOR
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Page/Page column 80, (2010/11/29)
A compound represented by general formula (I):A-B-D whereinA represents a substituted or unsubstituted 1-pyrrolidinyl group, a substituted or unsubstituted 3-thiazolidinyl group, a substituted or unsubstituted 1-oxo-3-thiazolidinyl group, or the like;B r
NEW COMPOUNDS
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Page/Page column 52, (2008/06/13)
The present invention provides new compounds of formula Ia and Ib: as well as a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
