• Title/Summary/Keyword: Isoquinoline

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Isoquinolines: Are they possible candidate for $Ca^{2+}$ blockers\ulcorner

  • 장기철;윤용진;조수동;정원석
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.217-217
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    • 1994
  • Calcium entry blockers, capable of inhibiting transmembrane influx of extracellular calcium through specific calcium channels, are useful drugs in the treatment of angina pectoris, hypertension, cardiac arrythmia, and various cardiovascular disorders. Compounds having isoquinoline structures have recently been reported to possess calcium antagonistic action. Therefore, in the present study, we have attempted to synthesize some isoquinoline and related compound.; in order to search for potentially effective chemicals acting on cardiovascular system, and evaluated their pharmacological properties focusing on calcium antagonistic actions. Almost all of the compounds so far synthesized, had inhibitory action against phenylephrine or high potassium-induced contraction in vascular smooth muscle with different degrees of potencies depending on their structures, However, some of tetrahydroisoquinoline analogs showed directly inhibit calcium current in isolated rabbit cardiac myocytes examined by patch clamp techniques. The pharmacological properties of these compounds need more intensive investigation as to whether these chemicals may have developed as a new cardiovascular active drugs. Therefore, we are now under investigation of the mechanism of action of these compounds.

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Cytotoxic Isoquinoline Alkaloids from Chelidonium majus var. asiaticum

  • Lee, Jun;Shon, Mi-Yae;Jang, Dae-Sik;Ha, Tae-Joung;Hwang, Seon-Woo;Nam, Sang-Hae;Seo, Eun-Kyoung;Park, Ki-Hun;Yang, Min-Suk
    • Journal of Applied Biological Chemistry
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    • v.48 no.4
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    • pp.198-201
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    • 2005
  • Two known isoquinoline alkaloids, (+)-chelidonine (1) and (-)-stylopine (2), were isolated from $CHCl_3$-soluble fraction of whole plants of Chelidonium majus L. var. asiaticum, and their structures were identified by spectroscopic methods and X-ray crystallographic analysis. Two isolates (1 and 2) were examined for their in vitro cytotoxic activities against five human cancer cell lines including DU-145 (prostate), MCF (breast), A549 (lung), HePG2 (liver), and HT-29 (colon) by sulphorhodamine B (SRB) assay.

Synthes is of 9,10-difluoro-5,6,6a,7,11b-pentahydroindano [2,1-c]isoquinoline (9,10- 디플루오르 -5,6,6a,7,11b- 펜타하이드로인다노[2,1-c] 이소퀴놀린의 합성)

  • Ma, Eun-Sook;Kim, Min-Jung
    • YAKHAK HOEJI
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    • v.44 no.6
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    • pp.505-510
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    • 2000
  • The synthesis of pentahydroindanoisoquinoline (4) compound has been achieved via the cyclization of 2-(N-benzylamino)-5,6-difluoro-1-indanol (10a, 10b), which was prepared by condensation and reduction of 2-amino-1-indanol and benzaldehyde in ethanol. The stereochemistry of $H_{6a}$ and $H_{11b}$ of 9,10-difluoro-5,6,6a,7,11b-pentahydroindano[2,1-c]isoquinoline (4) was the trans B/C ring fusion.

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Synthesis and Structure-Activity Relationship Studies of Substituted Isoquinoline Analogs Antitumor Agent

  • Cheon, Seung-Hoon;Park, Joon-Suck;Chung, Byung-Ho;Choi, Bo-Gil;Cho, Won-Jae;Choi, Sang-Un;Lee, Chong-Ock
    • Archives of Pharmacal Research
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    • v.21 no.2
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    • pp.193-197
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    • 1998
  • A number of substituted isoquinolin-1-ones, possible bioisosteres of the 5-aryl substituted 2,3-dihydroimidazo[2,$1-a$]isoquinolines, were synthesized and tested for their antitumor activity against five different human tumor cell lines. O-(3-hydroxyporpyl) substituted compound (15) exhibited the best antitumor activity which is 3-5 times better than 5-[$4^1$-(piperidinomethyl)phenyl]-2,3-dihydroimidazo[2,$1-a$]isoquinoline (1).

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Design, Syntheses and Biological Evaluations of Nonpeptidic Caspase 3 Inhibitors

  • Kim, Eun-Sook;Yoo, Sung-Eun;Yi, Kyu-Yang;Lee, Sun-Kyung;Noh, Jae-Sung;Jung, Yong-Sam;Kim, Eun-Hee;Jeong, Nak-Chul
    • Bulletin of the Korean Chemical Society
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    • v.23 no.7
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    • pp.1003-1010
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    • 2002
  • Caspase 3, a member of cysteine protease family, is well known as a major apoptosis effector and is involved in cell death as a result of ischemic diseases such as stroke and myocardial infarction, therefore the inhibition of caspase 3 may protect those apoptotic cell damages. During the high-throughput screening of the compounds from the Korea Chemical Bank, berberine derivatives (A and B), an isoquinoline alkaloid, have been identified as potential inhibitors for caspase 3. Based on this finding we carried out molecular modeling study to identify the pharmacophoric elements of berberine structure which interact with a substrate-recognition binding site of caspase 3 and came up with several novel scaffolds. In this report, we will discuss the molecular modeling, syntheses and the enzyme inhibitory activities of these novel compounds.

Isoquinoline Alkaloids from Fumaria bastardii

  • Kucukboyaci, Nurgun;Bingol, Funda;Sener, Bilge;Kutney, James P.;Stoynov, Nikolay
    • Natural Product Sciences
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    • v.4 no.4
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    • pp.257-262
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    • 1998
  • The extract of the aerial parts of Fumaria bastardii Bor. afforded 12 alkaloids belonging to the skeletally six different groups of the isoquinoline alkaloids. In this publication, the isolation and identification of protopine (1), corydaldine (2), oxyhydrastinine (3), (-)-fumaritine (4), (+)-fumariline (5), (-)-O-methylfumarophycine (12), (+)-bicuculline (10), $(-)-{\beta}-hydrastine$ (7), (-)-corlumine (11), (+)-tetrahydropalmatine (8), (-)-stylopine (6), and (+)-juziphine (9) are described. Their structures have been determined by using extensive spectroscopic techniques. This is the first report of the occurrence of these alkaloids in Fumaria bastardii of Turkish origin.

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