5666757926

P2.053

*41*001V

Synthesis of light-responsive MRI contrasł agents

Fneosrikd fl#eflmg.*» Marc C A Stuart,* Rud) A J O Oiorck*,'- Ben L. Fcrmga* and Wiktor S/ymartakl,**

• v>wv. S».v.rjC/Sfctrngft /rcmitff tor ChgmtUy, Urwisty o( GrOMtyM, “ Departmmi ot Rdótstogy. Uare/nty Mcdctt Ceniot Gmmtswi, Gw>«ga/t. f/*,i

Research goal

• Mtgmtic Rmoomk* imoę^ _tMRi ■$ an outsunong mecacal *tvtg«va tdcnnuyjo m to iU non-inv*»lvon®s» and e*c«ltent rtaotution fot anatomlc*l tmaging Ho^.-er. »f» tunctional ■nfonnatton c«anod trom MRI «llmited '

*9*«» tCA) thal a'B r«ponjr<e to kxal cnanges m i aic roeocd to osorcomc t*a Imtason. WSAareh ts to dcvclop Iight-rc$ponstve Uw uto ol lgnt-e(nirr.g targoting *Cwdisease t<s.»ue (Fięura i)

Design I

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Methods

mumcomponent reaction (MCfl» Ic contrast agorns. dmotoyrg a the ptKKoroipor.we mo*ry a* one cl lhe 2. vt>>o*)^: The f*<AŁv?/ bc*zrc aro aner Dy th© tóut>'i/łr^ of anchor.ng

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Bgi/e 3 Struclur# of compcund I

•    The first exampfe (compound I) presents an omphiphllic Qd>‘-4igand wbch m .ts infocf from • can Cc incorporatod mto hposomes

• Pnotocteawage łcads !o tho converslon of a macromolecular to a smali, gulckly tumDHng contrast

agent. *hicn changes refcudytiy

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Ccc ta V ajtf i wth aoywrfl

Groto lęołomoi

• •v^-G3^uctyTt>4«

T»gt/o 4 pnctoacovaton ot Wcotc ocord contrast agent

• The chcto/osponsf.c oc<e struduro »s zyrtfoyzcd usmg a Passenni MCR Subsecjuentiy, tre h/drophofre tai. funct&tt as an onchonng group for Iposomes rs artached via a cfick reaction, finały mę Ugand tor Go *• rs int/oductd

pęt

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pH. O.

Fn*jł*5 Syntheos ot cocrpognd I

CiyoTEM anałkrsis shn^fi th* cj

rrołtf..! nrirAB.

Design II

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solubllity awitch

Fguro 7 Structuro ofcompojn

•    The second design rofor. on solubiJity switch

•    Th© dtferont hydration States l activat.on rosult m differoni teUuMfy

•    Tho synlhottc route <s s milar lo lho or

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PK^jro tt Syntheois ot compound I

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