Solid-phase synthesis of 2,4-diaminoquinazolines

Wu, Zhengdong; Kim, Joo-young; Söll, Richard; Dhanoa, Dale

doi:10.1002/1097-0290(200021)71:2<87::aid-bit1>3.0.co;2-w

Cited by 3 publications

(2 citation statements)

References 13 publications

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“…Solid phase synthesis of 2,4-diaminoquinazolines (100) and (101) has been described in separate reports from Dhanoa [155] and Dener [156] respectively; a high degree of structural diversity was obtained in both studies.…”

Section: Miscellaneous Scaffoldsmentioning

confidence: 99%

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Design and Synthesis of Protein Superfamily-Targeted Chemical Libraries for Lead Identification and Optimization

Shuttleworth¹,

Connors²,

Fu³

et al. 2005

CMC

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This review chronicles original literature dating back to 1992 outlining the applications of parallel synthesis and combinatorial chemistry to the synthesis of compound libraries focused towards specific superfamilies of molecular targets. Target families that have received significant literature coverage include kinases, proteases, nuclear hormone receptors and cell surface receptors, notably GPCRs.

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Section: Miscellaneous Scaffoldsmentioning

confidence: 99%

“…The first four libraries were prepared to specifically examine each of the four positions located around the hydroxyl amine core; the final two libraries, synthesized simultaneously, were prepared to examine two separate areas of the chemical series. From this exercise a 4.3 nM inhibitor of plasmepsin II, (155), was identified.…”

Section: Aspartyl Proteasesmentioning

confidence: 99%

Design and Synthesis of Protein Superfamily-Targeted Chemical Libraries for Lead Identification and Optimization

Shuttleworth¹,

Connors²,

Fu³

et al. 2005

CMC

View full text Add to dashboard Cite

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Synthetic Approaches Towards Quinazolines, Quinazolinones and Quinazolinediones on Solid Phase

Vögtle¹,

Marzinzik²

2004

QSAR Comb. Sci.

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Full PaperQuinazolines are a pharmacologically very attractive class of compounds and have shown activity in various assays. Several successfully launched drugs are based on this scaffold. As a consequence, a more intensive exploitation in drug discovery by solid-phase syntheses of quinazoline libraries has been initiated. A diverse array of combinatorial quinazoline syntheses have been published and an increasing effort is to be expected in the near future to provide more efficient solid phase approaches towards quinazolines, quinazolinones and quinazolinediones. This review summarizes the literature published until January 2004 describing methods for synthesis and modification of these compounds on solid phase.

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Recent advances in the design and synthesis of prazosin derivatives

Minarini¹,

Bolognesi²,

Tumiatti³

et al. 2006

Expert Opinion on Drug Discovery

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Due to the large number of therapeutic indications, particularly for antagonists, a field of constant interest in medicinal chemistry is the design, synthesis and pharmacological evaluation of ligands that bind at α1-adrenoreceptors, which include α1a, α1b and α1d subtypes. This review, which is mainly based on literature over the past 10 years, focuses on the developments of some of the most potent, selective and widely used α1-adrenoreceptor antagonists that are structurally related to prazosin (which is characterised by a quinazoline moiety). Initially introduced in therapy for the management of hypertension, prazosin derivatives have become increasingly common in the treatment of benign prostatic hyperplasia. During the past few years, new perspectives have emerged for the use of these derivatives as a novel class of apoptosis-inducing agents in prostate cancer.

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Solid-phase synthesis of 2,4-diaminoquinazolines

Cited by 3 publications

References 13 publications

Design and Synthesis of Protein Superfamily-Targeted Chemical Libraries for Lead Identification and Optimization

Design and Synthesis of Protein Superfamily-Targeted Chemical Libraries for Lead Identification and Optimization

Synthetic Approaches Towards Quinazolines, Quinazolinones and Quinazolinediones on Solid Phase

Recent advances in the design and synthesis of prazosin derivatives

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