2-<4-(7-Methoxy-2-Methylbenzofuranyl)>-4-(3,4-Methylenedioxyphenyl)-4-Oxobutyronitrile置于吡啶,盐酸,Sodium Hydroxide,Sodium Tetrahydroborate,四氧化锇,氢气,四氯化钛,Potassium Carbonate,甲烷,对甲苯磺酸,过碘酸,2,3-二氯-5,6-二氰基-1,4-苯醌,Palladium Dichloride,三氯氧磷体系中,用 1,4-二氧六环,乙醇,氯仿,水,溶剂黄146,N,N-二甲基甲酰胺,乙腈,Xylene,苯 用作溶剂,25.0~60.0 °C,101.33 Kpa 条件下,反应 30.0H,反应生成白屈菜赤碱 参考文献:Studies On The Chemical Constituents Of Rutaceous Plants. Part Lxxiii. Total Synthesis Of Chelerythrine,A Benzo(C)Phenanthridine Alkaloid. 标题:Studies On The Chemical Constituents Of Rutaceous Plants. Part Lxxiii. Total Synthesis Of Chelerythrine,A Benzo(C)Phenanthridine Alkaloid. 摘要:利用我们的新颖合成方法,包括csf介导的芳基炔丙基醚克莱森重排为2-甲基苯并呋喃以及呋喃环氧化裂解为水杨醛,完成了苯并[c]菲啶生物碱白屈菜赤碱的全合成.通过图3所示的两条路线制备的共同中间体(5). Doi:10.1248/cpb.40.2002
专利号:US-2013331427-A1 优先权日:2006-07-28 标题:Methods of stimulating cellular growth, synaptic, remodeling and consolidation of long-term memory 发明人:ALKON DANIEL L 权利人:BRNI NEUROSCIENCES INST; BRNI NEUROSCIENCES INST 摘要:The present invention provides methods of slowing or reversing the loss of memory and learning comprising the steps of contacting an effective amount of a PKC activator with a protein kinase C (PKC) in a subject identified with memory loss slowing or reversing memory loss. The present invention provides methods of stimulating cellular growth, neuronal growth, dendritic growth, dendritic spine formation, dendritic spine density, and the translocation of ELAV to proximal dendrites, and synaptic remodeling. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC.
专利号:WO-9941984-A9 优先权日:1998-02-20 标 题 :INTERACTION BETWEEN THE MEC1-DEPENDENT DNA SYNTHESIS CHECKPOINT AND G1 CYCLIN FUNCTION IN $i(SACCAROMYCES CEREVISIAE) 发明人:VALLEN ELIZABETH A; CROSS FREDERICK R 权利人:HUTCHINSON FRED CANCER RES 摘要:The completion of DNA synthesis in yeast is monitored by a checkpoint that requires MEC1 and RAD53. Overexpression of the S. cerevisiae G1 cyclin CLN1 results in genomic instability and lethality of mec1-1 checkpoint-deficient cells compared to cln1 cln2 mec1-1 cells. Here we show that overexpression of CLN2 or CLB5, but not CLN3, also killed mec1-1 strains. We identified RNR1, which encodes a subunit of ribonucleotide reductase, as a high-copy suppressor of the lethality of mec1-1 GAL1-CLN1. Northern analysis demonstrated that RNR1 expression is reduced by CLN1 or CLN2 overexpression. Since limiting RNR1 expression might decrease dNTP pools, CLN1 or CLN2 may cause lethality in mec1-1 strains by causing initiation of DNA replication with inadequate dNTP pools. In MEC1 strains, a delay of S phase due to the checkpoint would occur, but in mec1-1 strains lethality would result. Consistent with this model, CLN1 overexpression did result in a prolongation of S phase in a MEC1 background. In a cln1 cln2 background, a prolonged period of expression of genes turned on at the G1-S border has been observed. Thus deletion of CLN1 and CLN2 could function similarly to overexpression of RNR1 in suppressing mec1-1 lethality. While Mec1p has been proposed to act in a linear pathway upstream of Rad53p, rad53 lethality was rescued little by deletion of CLN1 and CLN2, suggesting that Rad53p has Mec1-independent activities.
专利号:US-6399107-B1 优先权日:1998-12-22 标 题:Use of inhibitors of gag synthesis for the treatment of corneal haze 发明人:KESSLER TIMOTHY L; NIXON JON C; DAVID KAREN C; GRAFF GUSTAV 权利人:ALCON LAB INC 摘要:This invention relates to the compositions and methods for the treatment of corneal haze. The compositions and methods are particularly directed to the use of GAG synthesis inhibitors in the treatment of corneal haze.
专利号:EP-0354945-B1 优先权日:1988-01-13 标 题 :Process for the enhancement of enzyme activities and synthetic efficiency in microorganisms and higher plants 发明人:FIEDLER FRANZ; ZENK MEINHART H; GUNDLACH HEIDRUN; WEBER ALFRED; KENNECKE MARIO 权利人:SCHERING AG 摘要:In the process disclosed, the organisms are brought into contact witn inactivated elicitor-containing microorganisms, fragments of the latter, or excretions of elicitor-containing microorganisms. Only inactivated elicitor-containing bacteria, fragments of the latter, or excretions of elicitor-containing bacteria may be used to activate enzymes and promote synthesis in non-microbial organisms. The process can be used, for example, to promote synthesis in microorganisms or plants which produce pigments, antibiotics, alkaloids or phytoalexins or to activate enzymes in microorganisms capable of transforming steroids.
专利号:US-7989004-B2 优先权日:2004-05-27 标题:Antitubercular extracts of Salicornia brachiata 发明人:RATHOD MEENA RAJNIKANT; SHETHIA BHUPENDRA DHANVANTRAI; PANDYA JAYANT BATUKRAL; GHOSH PUSHPITO KUMAR; DODIA PRAKASH JAGIVANBHAL; SRIVASTAVA BRAHM S; SRIVASTAVA RANJANA; SRIVASTAVA ANIL; CHATURVEDI VINITA; VAIRAMANI MARIAPPANADAR 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to enhancement of anti-tubercular activity of active fraction isolated from Salicornia brachiata . The invention also discloses the non-toxic nature of the fraction and positively identifies Sucrose as its main constituent. Pure Sucrose is shown to have no anti-tubercular activity indicating thereby that activity of the fraction resides in one or more of the minor constituents. The minor constituents are shown to be relatively low molecular weight entities and a chromatographic technique is disclosed for separating them from the bulk sucrose to probe their activities and structures in detail, as also the possibility of their synthesis if the leads thrown up are novel.
专利号:US-2012276190-A1 优先权日:2009-08-28 标 题 :Therapy with a chimeric molecule and a pro-apoptotic agent 发明人:FITZGERALD DAVID J 权利人:FITZGERALD DAVID J; GOVERNMENT OF THE U S A AS REPRESENTED BY THE SECRETARY OF THE DEPT OF HEALTH & HUMAN SERVICES 摘要:The present invention provides compositions comprising a chimeric molecule comprising a cytotoxin that inhibits protein synthesis and an agent that inactivates an anti-apoptotic BCL-2 family member protein and methods of inhibiting the growth of or promoting the apoptosis of an aberrantly proliferating cell population by co-administering the chimeric molecule and the agent that inactivates an anti-apoptotic BCL-2 family member protein.
1: Yang T, Xu R, Su Q, Wang H, Liu F, Dai B, Wang B, Zhang Y. Chelerythrine hydrochloride inhibits proliferation and induces mitochondrial apoptosis in cervical cancer cells via PI3K/BAD signaling pathway. Toxicol In Vitro. 2020 Oct;68:104965. doi: 10.1016/j.tiv.2020.104965. Epub 2020 Aug 11. 17(10):1663. doi: 10.3390/ijms17101663. 3: Akhvlediani L, Koiava T, Lomtadze L, Joxadze M, Msxiladze L, Berashvili D, Bakuridze A. [COMPARATIVE ANALYSIS OF ANTIBACTERIAL EFFECT OF PHYTOANTIBIOTICS AND ANTIBIOTICS]. Georgian Med News. 2016 Nov;(Issue):79-86. Russian. 148:104368. doi: 10.1016/j.phrs.2019.104368. Epub 2019 Aug 12. Erratum in: Pharmacol Res. 2020 Jan 14;:104624. 535(1-3):228-33. doi: 10.1016/j.ejphar.2006.01.063. Epub 2006 Mar 3. 15(4):465-476. doi: 10.1007/s11302-019-09679-w. Epub 2019 Sep 13.
合成参考文献
参考文献:10.1186/1471-2180-10-49 摘要:Laskowski MC, Smulian AG. Insertional mutagenesis enables cleistothecial formation in a non-mating strain of Histoplasma capsulatum. BMC Microbiol. 2010 Feb 16;10():49.