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BMS-906024 is a drug with a [[benzodiazepine]] structure, developed by [[Bristol-Myers Squibb]] and disclosed at the spring 2013 [[American Chemical Society]] meeting in New Orleans to treat breast, lung, colon cancers and leukemia.<ref>{{cite web | vauthors = Drahl C | title = Liveblogging First-Time Disclosures of Drug Structures from #ACSNOLA | date = 2013 | url = http://cenblog.org/the-haystack/2013/04/liveblogging-first-time-disclosures-of-drug-structures-from-acsnola/ | work = Chemical and Engineering News | publisher = American Chemical Society }}</ref> The drug works as a pan-[[Notch signaling pathway|Notch]] inhibitor. The structure is one of a set patented in 2012,<ref>{{cite patent | country = WO | number = 2012129353 | title = Bisfluoroalkyl-1,4-Benzodiazepinone Compounds | inventor = Quesnelle C, Kim SH, Lee F, Gavai A | assign1 = Bristol-Myers Squibb Company | pubdate = 27 September 2012 | url = http://patentscope.wipo.int/search/en/detail.jsf?docId=WO2012129353 }}</ref> and is being studied in clinical trials.<ref name="pmid26005526">{{cite journal | vauthors = Gavai AV, Quesnelle C, Norris D, Han WC, Gill P, Shan W, Balog A, Chen K, Tebben A, Rampulla R, Wu DR, Zhang Y, Mathur A, White R, Rose A, Wang H, Yang Z, Ranasinghe A, D'Arienzo C, Guarino V, Xiao L, Su C, Everlof G, Arora V, Shen DR, Cvijic ME, Menard K, Wen ML, Meredith J, Trainor G, Lombardo LJ, Olson R, Baran PS, Hunt JT, Vite GD, Fischer BS, Westhouse RA, Lee FY | display-authors = 6 | title = Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors | journal = ACS Medicinal Chemistry Letters | volume = 6 | issue = 5 | pages = 523–7 | date = May 2015 | pmid = 26005526 | pmc = 4434460 | doi = 10.1021/acsmedchemlett.5b00001 }}</ref><ref name="pmid28978720">{{cite journal | vauthors = Morgan KM, Fischer BS, Lee FY, Shah JJ, Bertino JR, Rosenfeld J, Singh A, Khiabanian H, Pine SR | display-authors = 6 | title = Gamma Secretase Inhibition by BMS-906024 Enhances Efficacy of Paclitaxel in Lung Adenocarcinoma | journal = Molecular Cancer Therapeutics | volume = 16 | issue = 12 | pages = 2759–2769 | date = December 2017 | pmid = 28978720 | pmc = 5716926 | doi = 10.1158/1535-7163.MCT-17-0439 }}</ref><ref name="pmid30464927">{{cite journal | vauthors = Sosa Iglesias V, Theys J, Groot AJ, Barbeau LM, Lemmens A, Yaromina A, Losen M, Houben R, Dubois L, Vooijs M | display-authors = 6 | title = Synergistic Effects of NOTCH/γ-Secretase Inhibition and Standard of Care Treatment Modalities in Non-small Cell Lung Cancer Cells | journal = Frontiers in Oncology | volume = 8 | pages = 460 | date = 2018 | pmid = 30464927 | pmc = 6234899 | doi = 10.3389/fonc.2018.00460 | doi-access = free }}</ref>
BMS-906024 is a drug with a [[benzodiazepine]] structure, developed by [[Bristol-Myers Squibb]] and disclosed at the spring 2013 [[American Chemical Society]] meeting in New Orleans to treat breast, lung, colon cancers and leukemia.<ref>{{cite web | vauthors = Drahl C | title = Liveblogging First-Time Disclosures of Drug Structures from #ACSNOLA | date = 2013 | url = http://cenblog.org/the-haystack/2013/04/liveblogging-first-time-disclosures-of-drug-structures-from-acsnola/ | work = Chemical and Engineering News | publisher = American Chemical Society }}</ref> The drug works as a pan-[[Notch signaling pathway|Notch]] inhibitor. The structure is one of a set patented in 2012,<ref>{{cite patent | country = WO | number = 2012129353 | title = Bisfluoroalkyl-1,4-Benzodiazepinone Compounds | inventor = Quesnelle C, Kim SH, Lee F, Gavai A | assign1 = Bristol-Myers Squibb Company | pubdate = 27 September 2012 | url = http://patentscope.wipo.int/search/en/detail.jsf?docId=WO2012129353 }}</ref> and is being studied in clinical trials.<ref name="pmid26005526">{{cite journal | vauthors = Gavai AV, Quesnelle C, Norris D, Han WC, Gill P, Shan W, Balog A, Chen K, Tebben A, Rampulla R, Wu DR, Zhang Y, Mathur A, White R, Rose A, Wang H, Yang Z, Ranasinghe A, D'Arienzo C, Guarino V, Xiao L, Su C, Everlof G, Arora V, Shen DR, Cvijic ME, Menard K, Wen ML, Meredith J, Trainor G, Lombardo LJ, Olson R, Baran PS, Hunt JT, Vite GD, Fischer BS, Westhouse RA, Lee FY | display-authors = 6 | title = Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors | journal = ACS Medicinal Chemistry Letters | volume = 6 | issue = 5 | pages = 523–7 | date = May 2015 | pmid = 26005526 | pmc = 4434460 | doi = 10.1021/acsmedchemlett.5b00001 }}</ref><ref name="pmid28978720">{{cite journal | vauthors = Morgan KM, Fischer BS, Lee FY, Shah JJ, Bertino JR, Rosenfeld J, Singh A, Khiabanian H, Pine SR | display-authors = 6 | title = Gamma Secretase Inhibition by BMS-906024 Enhances Efficacy of Paclitaxel in Lung Adenocarcinoma | journal = Molecular Cancer Therapeutics | volume = 16 | issue = 12 | pages = 2759–2769 | date = December 2017 | pmid = 28978720 | pmc = 5716926 | doi = 10.1158/1535-7163.MCT-17-0439 }}</ref><ref name="pmid30464927">{{cite journal | vauthors = Sosa Iglesias V, Theys J, Groot AJ, Barbeau LM, Lemmens A, Yaromina A, Losen M, Houben R, Dubois L, Vooijs M | display-authors = 6 | title = Synergistic Effects of NOTCH/γ-Secretase Inhibition and Standard of Care Treatment Modalities in Non-small Cell Lung Cancer Cells | journal = Frontiers in Oncology | volume = 8 | pages = 460 | date = 2018 | pmid = 30464927 | pmc = 6234899 | doi = 10.3389/fonc.2018.00460 | doi-access = free }}</ref>

{{benzodiazepines}}

== References ==
== References ==
{{Reflist|30em}}
{{Reflist|30em}}
{{benzodiazepines}}




[[Category:Benzodiazepines]]
[[Category:Benzodiazepines]]

Latest revision as of 14:14, 4 February 2023

BMS-906024
Identifiers
  • (2R,3S)-N-[(3S)-1-Methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]-2,3-bis(3,3,3-trifluoropropyl)succinamide
CAS Number
PubChem CID
PubChem SID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC26H26F6N4O3
Molar mass556.509 g·mol−1
3D model (JSmol)
  • CN1c2ccccc2C(=N[C@@H](C1=O)NC(=O)[C@H](CCC(F)(F)F)[C@H](CCC(F)(F)F)C(=O)N)c3ccccc3
  • InChI=1S/C26H26F6N4O3/c1-36-19-10-6-5-9-18(19)20(15-7-3-2-4-8-15)34-22(24(36)39)35-23(38)17(12-14-26(30,31)32)16(21(33)37)11-13-25(27,28)29/h2-10,16-17,22H,11-14H2,1H3,(H2,33,37)(H,35,38)/t16-,17+,22+/m0/s1
  • Key:AYOUDDAETNMCBW-GSHUGGBRSA-N

BMS-906024 is a drug with a benzodiazepine structure, developed by Bristol-Myers Squibb and disclosed at the spring 2013 American Chemical Society meeting in New Orleans to treat breast, lung, colon cancers and leukemia.[1] The drug works as a pan-Notch inhibitor. The structure is one of a set patented in 2012,[2] and is being studied in clinical trials.[3][4][5]

References

[edit]
  1. ^ Drahl C (2013). "Liveblogging First-Time Disclosures of Drug Structures from #ACSNOLA". Chemical and Engineering News. American Chemical Society.
  2. ^ WO 2012129353, Quesnelle C, Kim SH, Lee F, Gavai A, "Bisfluoroalkyl-1,4-Benzodiazepinone Compounds", published 27 September 2012, assigned to Bristol-Myers Squibb Company 
  3. ^ Gavai AV, Quesnelle C, Norris D, Han WC, Gill P, Shan W, et al. (May 2015). "Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors". ACS Medicinal Chemistry Letters. 6 (5): 523–7. doi:10.1021/acsmedchemlett.5b00001. PMC 4434460. PMID 26005526.
  4. ^ Morgan KM, Fischer BS, Lee FY, Shah JJ, Bertino JR, Rosenfeld J, et al. (December 2017). "Gamma Secretase Inhibition by BMS-906024 Enhances Efficacy of Paclitaxel in Lung Adenocarcinoma". Molecular Cancer Therapeutics. 16 (12): 2759–2769. doi:10.1158/1535-7163.MCT-17-0439. PMC 5716926. PMID 28978720.
  5. ^ Sosa Iglesias V, Theys J, Groot AJ, Barbeau LM, Lemmens A, Yaromina A, et al. (2018). "Synergistic Effects of NOTCH/γ-Secretase Inhibition and Standard of Care Treatment Modalities in Non-small Cell Lung Cancer Cells". Frontiers in Oncology. 8: 460. doi:10.3389/fonc.2018.00460. PMC 6234899. PMID 30464927.