• Title/Summary/Keyword: Pyrazoles

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Synthesis and Biological Activity of New 4-(Pyridin-4-yl)-(3-methoxy-5-methylphenyl)-1H-pyrazoles Derivatives as ROS Receptor Tyrosine Kinase Inhibitors

  • Park, Byung Sun;El-Deeb, Ibrahim M.;Yoo, Kyung Ho;Han, Dong Keun;Tae, Jin Sung;Lee, So Ha
    • Bulletin of the Korean Chemical Society
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    • v.33 no.11
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    • pp.3629-3634
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    • 2012

  • A series of new 4-(pyridin-4-yl)-(3-methoxy-5-methylphenyl)-1H-pyrazoles (6a-k & 7a-l) has been rationally designed based on the structure of the lead compound KIST301080, a selective ROS receptor tyrosine kinase inhibitor, in order to study the activity of ROS of this new class of inhibitors. The compounds were synthesized and screened against ROS kinase, where compound 6h showed moderate inhibitory activity with an $IC_{50}$ value of $6.25{\mu}M$. The study emphasized the importance of the acetonitrile group at the pyrazole ring and also the importance of having a hydrogen bond donor on the distal phenyl ring linked to the pyridine moiety.

  • https://doi.org/10.5012/bkcs.2012.33.11.3629 인용 PDF KSCI

Synthesis of Some New 4H-(Pyrano and/or Piperidino)[3,2-d] Pyazoles and Pyrazolo[5,4-d] Thiopyrans

  • Etman, H.A.;El-Ahl, A.S.;Metwally, M.A.
    • Archives of Pharmacal Research
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    • v.17 no.4
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    • pp.278-280
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    • 1994

  • 1,5-diketones(3) undewent cyclization to 4H-pyrano[3,2-d]pyrazoles (4a-d),4H-piperidino[3, 2-d]pyrazole (5) and pyrazolo[5,4-d]thiopyran (6) upon treatment with P/sub 2/O/sub 5/, CH/sub 3/COONH/sub 4/ and /or P/sub 2/S/sub 5/. Moreover, treatment of (4) with CH/sub 3/COONH/sub 4/ and/or P/sub 2/S/sub 5/ afforded (5) and (6). The structures of the hitherto unknown ring systems have been confirmed by analytical and spectral data.

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Regioselective Synthesis of 1,3,4,5-Tetrasubstituted Pyrazoles from α-Alkenyl-α,β-Enones Derived from Morita-Baylis-Hillman Adducts

  • Kim, Sung Hwan;Lim, Jin Woo;Yu, Jin;Kim, Jae Nyoung
    • Bulletin of the Korean Chemical Society
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    • v.34 no.10
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    • pp.2915-2920
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    • 2013

  • Convenient synthetic method for 4-arylethylpyrazoles and 4-styrylpyrazoles was developed using ${\alpha}$-alkenyl-${\alpha},{\beta}$-enones readily accessed from the Morita-Baylis-Hillman reaction. For the synthesis of 4-arylethylpyrazole, the reactions with arylhydrazines needed to be carried out in o-dichlorobenzene under $N_2$ balloon atmosphere. On the other hand, 4-styrylpyrazoles required the reactions in ethanol under $O_2$ balloon atmosphere.

  • https://doi.org/10.5012/bkcs.2013.34.10.2915 인용 PDF KSCI

Design, Synthesis and in-vitro Screening of New 1H-Pyrazole and 1,2-Isoxazole Derivatives as Potential Inhibitors for ROS and MAPK14 Kinases

  • Al-Sanea, Mohammad M.;El-Deeb, Ibrahim M.;Lee, So Ha
    • Bulletin of the Korean Chemical Society
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    • v.34 no.2
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    • pp.437-442
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    • 2013

  • A new series of 4-(2-(substituted)pyridin-4-yl)-3-(3-methoxy-5-methylphenyl)-1H-pyrazoles (4a-f) and their 1,2-isoxazole analogues (5a-f) has been rationally designed, synthesized and screened against both ROS and MAPK14 kinases. Compounds 4b, 4c and 4e showed moderate inhibitions against both ROS and MAPK14 kinases. Compound 4e has showed the strongest inhibitions with IC50 values of 1.25 ${\mu}M$ and 3.00 ${\mu}M$ against ROS and MAPK14 kinases, respectively. A brief structure-activity relationship study and a molecular modeling study were made revealing a group of essential structural features for good kinase inhibitory activity within this new class of kinase inhibitors.

  • https://doi.org/10.5012/bkcs.2013.34.2.437 인용 PDF KSCI

Synthesis of new pyrazoles and their herbicidal effects (새로운 pyrazole 유도체의 합성과 제초활성)

  • Jeon, Dong-Ju;Lee, Jung-No;Kim, Hyung-Rae;Song, Jong-Hwan;Hwang, In-Taek;Ryu, Eung-K.
    • The Korean Journal of Pesticide Science
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    • v.3 no.1
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    • pp.96-101
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    • 1999

  • 3-Trifluoromethylpyrazoles and 4-benzenecarbinolpyrazoles were prepared by the new synthetic methodologies, and their herbicidal effects were tested (in vivo) in the upland conditions and in the flooded paddy conditions for the purpose of the development of new herbicides. In upland conditions, most of the pyrazoles showed weak herbicidal effects at 4 kg/ha dosage in the post-emergence test, while no herbicidal effects in the pre-emergence test. In the flooded paddy conditions, some of the pyrazoles showed good herbicidal effects at a rate of 4 kg/ha, especially, 3-trifluoromethyl-4-(4-methoxybenzoyl)pyrazole showed the best herbicidal activity with good selectivity between rice and weeds. But other derivatives substituted with electron-donating groups such as dior trimethoxy and sulfides, and 4-benzenecarbinolpyrazoles showed weak herbicidal effects.

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