General Information of Drug (ID: DM8OC9F)

Drug Name
Pergularinine Drug Info
Synonyms
Tylophorinine; TYLOPHORININE; CHEMBL398325; 571-70-0; NSC100055; AC1L6CHR; (13as,14r)-3,6,7-trimethoxy-9,11,12,13,13a,14-hexahydrodibenzo[f,h]pyrrolo[1,2-b]isoquinolin-14-ol; AC1Q57Z0; CTK5A6391; Dibenzo(f,h)pyrrolo(1,2-b)isoquinolin-14-ol, 9,11,12,13,13a,14-hexahydro-3,6,7-trimethoxy-, (13aS-cis)-; BDBM50213934; NSC-100055; NCI60_000003; (13aS,14R)-3,6,7-trimethoxy-9,11,12,13,13a,14-hexahydrophenanthro[9,10-f]indolizin-14-ol; Dibenzo[f,h]pyrrolo[1,2-b]isoquinolin-14-ol,9,11,12,13,13a,14-hexahydro-3,6,7-trimethoxy-,
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1] , [2]
Cross-matching ID
PubChem CID
264751
CAS Number
CAS 571-70-0
TTD Drug ID
DM8OC9F

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Investigative Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
[(R)-(+)-deoxytylophorinidine DMPFUBE Discovery agent N.A. Investigative [2]
ISIS 10582 DMB5F9H Discovery agent N.A. Investigative [3]
DCB-3503 DMPRYTW Discovery agent N.A. Investigative [2]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Proguanil DMBL79I Malaria 1F40-1F45 Approved [4]
Meprobamate DMHM93Y Anxiety disorder 6B00-6B0Z Approved [5]
Pralatrexate DMAO80I Breast cancer 2C60-2C65 Approved [6]
Ustekinumab DMHTYK3 Plaque psoriasis EA90.0 Approved [7]
Trimetrexate DMDEA85 Toxoplasmosis 1F57 Approved [8]
MCB-3837 DM0R4Z5 Malaria 1F40-1F45 Approved [5]
Chlorproguanil DM1IFGT Malaria 1F40-1F45 Approved [5]
LY333531 DMGMC8H Solid tumour/cancer 2A00-2F9Z Phase 2 [9]
Metoprine DM5GQD7 Advanced cancer 2A00-2F9Z Phase 2 [10]
Aminopterin DMQ9RBV leukaemia 2A60-2B33 Withdrawn from market [11]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
c-Jun messenger RNA (c-Jun mRNA) TTS7IR5 JUN_HUMAN Inhibitor [2]
Polypeptide deformylase (PDF) TT9SL3Q DEFM_HUMAN Inhibitor [1]

References

1 Inhibition of dihydrofolate reductase and cell growth activity by the phenanthroindolizidine alkaloids pergularinine and tylophorinidine: the in vitro cytotoxicity of these plant alkaloids and their potential as antimicrobial and anticancer agents. Toxicol In Vitro. 2000 Feb;14(1):53-9.
2 Structure-activity studies of phenanthroindolizidine alkaloids as potential antitumor agents. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4338-42.
3 US patent application no. 6,312,900, Antisense oligonucleotide compositions and methods for the modulation of activating protein 1.
4 Transformation with human dihydrofolate reductase renders malaria parasites insensitive to WR99210 but does not affect the intrinsic activity of proguanil. Proc Natl Acad Sci U S A. 1997 Sep 30;94(20):10931-6.
5 The fight against drug-resistant malaria: novel plasmodial targets and antimalarial drugs. Curr Med Chem. 2008;15(2):161-71.
6 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
7 Novel Saccharomyces cerevisiae screen identifies WR99210 analogues that inhibit Mycobacterium tuberculosis dihydrofolate reductase. Antimicrob Agents Chemother. 2002 Nov;46(11):3362-9.
8 Expression and characterization of recombinant human-derived Pneumocystis carinii dihydrofolate reductase. Antimicrob Agents Chemother. 2000 Nov;44(11):3092-6.
9 Three-dimensional structure of M. tuberculosis dihydrofolate reductase reveals opportunities for the design of novel tuberculosis drugs. J Mol Biol. 2000 Jan 14;295(2):307-23.
10 Mutant Gly482 and Thr482 ABCG2 mediate high-level resistance to lipophilic antifolates. Cancer Chemother Pharmacol. 2006 Dec;58(6):826-34.
11 Loss of folylpoly-gamma-glutamate synthetase activity is a dominant mechanism of resistance to polyglutamylation-dependent novel antifolates in multiple human leukemia sublines. Int J Cancer. 2003 Feb 20;103(5):587-99.