- Novel sulfone amide derivatives compound, Manufacturing method thereof, Phamaceutical composition for preventing and treating cancer containing the same, and Methods for preventing and treating cancer using the same
-
The present invention relates to novel sulfonamide-based derivatives, a manufacturing method thereof, and to a pharmaceutical composition comprising the same for preventing or treating cancer. More particularly, the novel sulfonamide-based derivatives target Rab27a, and hinder or suppress expression of the Rab27a. Also, the present invention relates to a method for preventing or treating cancer using the pharmaceutical composition.
- -
-
Paragraph 0061-0066
(2019/12/03)
-
- Inhibition of cancer cell invasion by new ((3,4-dihydroxy benzylidene)hydrazinyl)pyridine-3-sulfonamide analogs
-
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.
- 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)
-
- PYRROLOPYRIMIDINE COMPOUNDS AND USES THEREOF
-
The present disclosure provides pyrrolopyrimidine compounds and methods of use therefor. For example, the disclosure provides certain pyrrolopyrimidine compounds capable of inhibiting JAK kinases. The disclosure further provides the pharmaceutical compositions containing these pyrrolopyrimidine compounds, and use of these pyrrolopyrimidine compounds in the treatment of disorders or diseases, such as inflammatory diseases and cancer.
- -
-
Paragraph 0326; 0327
(2013/08/28)
-
- PYRROLOPYRIMIDINE COMPOUNDS AND USES THEREOF
-
Disclosed are pyrrolopyrimidine compounds of formula (I) capable of inhibiting JAK kinase, wherein R1, R2 and m are defined as in the description. The pharmaceutical compositions containing said pyrrolopyrimidine compounds and uses of said pyrrolopyrimidine compounds in the treatment of disorders or diseases such as inflammatory diseases and cancers are also disclosed.
- -
-
Page/Page column 83; 84
(2012/03/10)
-
- PYRROLOPYRIMIDINE COMPOUNDS AND USES THEREOF
-
The present invention provides pyrrolopyrimidine compounds and methods of use therefor. In particular, the invention provides certain pyrrolopyrimidine compounds having the activity of inhibiting JAK kinases. The invention also provides the pharmaceutical compositions containing these pyrrolopyrimidine compounds and use of these compounds in the treatment of inflammatory diseases and cancer.
- -
-
Page/Page column 74-75
(2012/03/10)
-
- DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF AS HIF ACTIVATORS
-
The present invention relates to novel substituted dihydropyrazolone derivatives, to their preparation and to their therapeutic use as activators of the transcription factor HIF.
- -
-
Page/Page column 17
(2011/12/13)
-
- DIPEPTIDYL PEPTIDASE IV INHIBITOR
-
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
- -
-
Page/Page column 79-80
(2010/11/29)
-